DGIdb - TRAMETINIB Drug Record

TRAMETINIB chembl:CHEMBL2103875 ApprovedAntineoplastic

Alternate Names:

MEKINIST
GSK-1120212
JTP-74057
JTP 74057
GSK1120212
TRAMETINIB
TRAMETINIBUM
GSK212
MEKINIST®
TRAMETINIB DIMETHYL SULFOXIDE
GSK 1120212
GSK1120212B
TMT212
TRAMÉTINIB
pubchem.compound:11707110
drugbank:08911
chemidplus:871700-17-3
rxcui:1425099
chembl:CHEMBL2103875

Drug Info:

FDA Approval	Melanoma (with BRAF V600 mutation)
Notes	allosteric inhibitor
Drug Class	Kinase Inhibitors
FDA Approval	not approved
Drug Class	Small molecule
Drug Indications	antineoplastic agent

(11 More Sources)

Publications:

Ambrosini et al., 2014, Overexpression of DDX43 mediates MEK inhibitor resistance through RAS Upregulation in uveal melanoma cells., Mol. Cancer Ther.
Imielinski et al., 2014, Oncogenic and sorafenib-sensitive ARAF mutations in lung adenocarcinoma., J. Clin. Invest.
Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.
Salama et al., 2013, Trametinib (GSK1120212) in the treatment of melanoma., Expert Opin Pharmacother
Diamond et al., 2016, Diverse and Targetable Kinase Alterations Drive Histiocytic Neoplasms., Cancer Discov
Russo et al., 2016, Tumor Heterogeneity and Lesion-Specific Response to Targeted Therapy in Colorectal Cancer., Cancer Discov
Carlino et al., 2015, Preexisting MEK1P124 mutations diminish response to BRAF inhibitors in metastatic melanoma patients., Clin. Cancer Res.
Greger et al., 2012, Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations., Mol. Cancer Ther.
Gannon et al., 2016, Identification of an "Exceptional Responder" Cell Line to MEK1 Inhibition: Clinical Implications for MEK-Targeted Therapy., Mol. Cancer Res.
Wagle et al., 2014, MAP kinase pathway alterations in BRAF-mutant melanoma patients with acquired resistance to combined RAF/MEK inhibition., Cancer Discov
Brammeld et al., 2017, Genome-wide chemical mutagenesis screens allow unbiased saturation of the cancer genome and identification of drug resistance mutations., Genome Res.
Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov
Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
Ahronian et al., 2015, Clinical Acquired Resistance to RAF Inhibitor Combinations in BRAF-Mutant Colorectal Cancer through MAPK Pathway Alterations., Cancer Discov
Nelson DS et al., 2015, MAP2K1 and MAP3K1 mutations in Langerhans cell histiocytosis., Genes Chromosomes Cancer
Brown NA et al., 2014, High prevalence of somatic MAP2K1 mutations in BRAF V600E-negative Langerhans cell histiocytosis., Blood
Gandara et al., 2017, A Phase 1/1b Study Evaluating Trametinib Plus Docetaxel or Pemetrexed in Patients With Advanced Non-Small Cell Lung Cancer., J Thorac Oncol
Sun et al., 2014, Intrinsic resistance to MEK inhibition in KRAS mutant lung and colon cancer through transcriptional induction of ERBB3., Cell Rep
Jing et al., 2012, Comprehensive predictive biomarker analysis for MEK inhibitor GSK1120212., Mol. Cancer Ther.
Infante et al., 2014, A randomised, double-blind, placebo-controlled trial of trametinib, an oral MEK inhibitor, in combination with gemcitabine for patients with untreated metastatic adenocarcinoma of the pancreas., Eur. J. Cancer
Ball et al., 2015, Trametinib with and without pazopanib has potent preclinical activity in thyroid cancer., Oncol. Rep.
Beadnell et al., 2016, The Mitogen-Activated Protein Kinase Pathway Facilitates Resistance to the Src Inhibitor Dasatinib in Thyroid Cancer., Mol. Cancer Ther.
Yamaguchi et al., 2016, A synthetic-lethality RNAi screen reveals an ERK-mTOR co-targeting pro-apoptotic switch in PIK3CA+ oral cancers., Oncotarget
Lin et al., 2015, The Hippo effector YAP promotes resistance to RAF- and MEK-targeted cancer therapies., Nat. Genet.
Infante et al., 2012, Safety, pharmacokinetic, pharmacodynamic, and efficacy data for the oral MEK inhibitor trametinib: a phase 1 dose-escalation trial., Lancet Oncol.
Dhawan et al., 2016, Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling., Nature
Peng et al., 2015, Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers., Cancer Cell
Manchado et al., 2016, A combinatorial strategy for treating KRAS-mutant lung cancer., Nature
Ziemke et al., 2016, Sensitivity of KRAS-Mutant Colorectal Cancers to Combination Therapy That Cotargets MEK and CDK4/6., Clin. Cancer Res.
Lu et al., 2017, Engineering and Functional Characterization of Fusion Genes Identifies Novel Oncogenic Drivers of Cancer., Cancer Res.
Drobysheva et al., 2017, Targeted MAPK Pathway Inhibitors in Patients With Disseminated Pilocytic Astrocytomas., J Natl Compr Canc Netw
Corcoran et al., 2015, Combined BRAF and MEK Inhibition With Dabrafenib and Trametinib in BRAF V600-Mutant Colorectal Cancer., J. Clin. Oncol.
Shi et al., 2014, A novel AKT1 mutant amplifies an adaptive melanoma response to BRAF inhibition., Cancer Discov
Long et al., 2016, Overall Survival and Durable Responses in Patients With BRAF V600-Mutant Metastatic Melanoma Receiving Dabrafenib Combined With Trametinib., J. Clin. Oncol.
Shen et al., 2016, Loss of cohesin complex components STAG2 or STAG3 confers resistance to BRAF inhibition in melanoma., Nat. Med.
2016, Triple Therapy Improves Colorectal Cancer Response., Cancer Discov
Kotschy et al., 2016, The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models., Nature
Kim et al., 2013, Phase II study of the MEK1/MEK2 inhibitor Trametinib in patients with metastatic BRAF-mutant cutaneous melanoma previously treated with or without a BRAF inhibitor., J. Clin. Oncol.
Marconcini et al., 2017, Metastatic BRAF K601E-mutated melanoma reaches complete response to MEK inhibitor trametinib administered for over 36 months., Exp Hematol Oncol
Joshi et al., 2015, Trametinib with or without vemurafenib in BRAF mutated non-small cell lung cancer., PLoS ONE
Chen et al., 2016, Oncogenic BRAF Deletions That Function as Homodimers and Are Sensitive to Inhibition by RAF Dimer Inhibitor LY3009120., Cancer Discov
Flaherty et al., 2012, Improved survival with MEK inhibition in BRAF-mutated melanoma., N. Engl. J. Med.
Long et al., 2014, Combined BRAF and MEK inhibition versus BRAF inhibition alone in melanoma., N. Engl. J. Med.
Long GV et al., 2017 Sep 10, Adjuvant Dabrafenib plus Trametinib in Stage III BRAF-Mutated Melanoma., N Engl J Med
Yu et al., 2015, Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092., PLoS ONE
Lange et al., 2014, Biological and molecular effects of small molecule kinase inhibitors on low-passage human colorectal cancer cell lines., Biomed Res Int
Waizenegger et al., 2016, A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation., Mol. Cancer Ther.
Klempner et al., 2016, BRAFV600E Mutations in High-Grade Colorectal Neuroendocrine Tumors May Predict Responsiveness to BRAF-MEK Combination Therapy., Cancer Discov
Agarwal et al., 2016, Response to Targeted Therapy in BRAF Mutant Anaplastic Thyroid Cancer., J Natl Compr Canc Netw
Schreuer et al., 2017, Combination of dabrafenib plus trametinib for BRAF and MEK inhibitor pretreated patients with advanced BRAF(V600)-mutant melanoma: an open-label, single arm, dual-centre, phase 2 clinical trial., Lancet Oncol.
Peh et al., 2016, The Combination of Vemurafenib and Procaspase-3 Activation Is Synergistic in Mutant BRAF Melanomas., Mol. Cancer Ther.
Gibson et al., 2017, Genomic Heterogeneity and Exceptional Response to Dual Pathway Inhibition in Anaplastic Thyroid Cancer., Clin. Cancer Res.
Falchook et al., 2012, Activity of the oral MEK inhibitor trametinib in patients with advanced melanoma: a phase 1 dose-escalation trial., Lancet Oncol.
Teh et al., 2016, An In Vivo Reporter to Quantitatively and Temporally Analyze the Effects of CDK4/6 Inhibitor-Based Therapies in Melanoma., Cancer Res.
Dahlman et al., 2012, BRAF(L597) mutations in melanoma are associated with sensitivity to MEK inhibitors., Cancer Discov
Yao et al., 2017, Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS., Nature
Isaacson AL et al., 2019, Urothelial carcinoma with an <i>NRF1-BRAF</i> rearrangement and response to targeted therapy., Cold Spring Harb Mol Case Stud
Aguirre AJ et al., 2018, Real-time Genomic Characterization of Advanced Pancreatic Cancer to Enable Precision Medicine., Cancer Discov
Long GV et al., 2014, Increased MAPK reactivation in early resistance to dabrafenib/trametinib combination therapy of BRAF-mutant metastatic melanoma., Nat Commun
Ross et al., 2016, The distribution of BRAF gene fusions in solid tumors and response to targeted therapy., Int. J. Cancer
Bowyer et al., 2014, Activity of trametinib in K601E and L597Q BRAF mutation-positive metastatic melanoma., Melanoma Res.
Larkin et al., 2014, Combined vemurafenib and cobimetinib in BRAF-mutated melanoma., N. Engl. J. Med.
Hutchinson et al., 2013, BRAF fusions define a distinct molecular subset of melanomas with potential sensitivity to MEK inhibition., Clin. Cancer Res.
Subbiah V et al., 2018, Dabrafenib and Trametinib Treatment in Patients With Locally Advanced or Metastatic BRAF V600-Mutant Anaplastic Thyroid Cancer., J Clin Oncol
Flaherty et al., 2012, Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations., N. Engl. J. Med.
Corcoran RB et al., 2018, Combined BRAF, EGFR, and MEK Inhibition in Patients with <i>BRAF</i><sup>V600E</sup>-Mutant Colorectal Cancer., Cancer Discov
Robert et al., 2015, Improved overall survival in melanoma with combined dabrafenib and trametinib., N. Engl. J. Med.
Planchard et al., 2016, Dabrafenib plus trametinib in patients with previously treated BRAF(V600E)-mutant metastatic non-small cell lung cancer: an open-label, multicentre phase 2 trial., Lancet Oncol.
Menzies et al., 2014, Dabrafenib and trametinib, alone and in combination for BRAF-mutant metastatic melanoma., Clin. Cancer Res.
Müller-Gärtner et al., 1989, [Long-term results following surgery or radioiodine treatment of solitary autonomous adenoma of the thyroid gland]., Chirurg
Bahadoran et al., 2013, Major clinical response to a BRAF inhibitor in a patient with a BRAF L597R-mutated melanoma., J. Clin. Oncol.
Dienstmann et al., 2015, Database of genomic biomarkers for cancer drugs and clinical targetability in solid tumors., Cancer Discov
Nicolaides et al., 2011, Targeted therapy for BRAFV600E malignant astrocytoma., Clin. Cancer Res.
Hoftijzer et al., 2009, Beneficial effects of sorafenib on tumor progression, but not on radioiodine uptake, in patients with differentiated thyroid carcinoma., Eur. J. Endocrinol.
Rad et al., 2013, A genetic progression model of Braf(V600E)-induced intestinal tumorigenesis reveals targets for therapeutic intervention., Cancer Cell
Maldonado et al., 2003, Determinants of BRAF mutations in primary melanomas., J. Natl. Cancer Inst.
Yang et al., 2012, Antitumor activity of BRAF inhibitor vemurafenib in preclinical models of BRAF-mutant colorectal cancer., Cancer Res.
Villanueva et al., 2010, Acquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by cotargeting MEK and IGF-1R/PI3K., Cancer Cell
Tiacci et al., 2011, BRAF mutations in hairy-cell leukemia., N. Engl. J. Med.
Sosman et al., 2012, Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib., N. Engl. J. Med.
Brose et al., 2002, BRAF and RAS mutations in human lung cancer and melanoma., Cancer Res.
Gupta-Abramson et al., 2008, Phase II trial of sorafenib in advanced thyroid cancer., J. Clin. Oncol.
Ho et al., 2013, Selumetinib-enhanced radioiodine uptake in advanced thyroid cancer., N. Engl. J. Med.
Rizzo et al., 2010, Prognostic vs predictive molecular biomarkers in colorectal cancer: is KRAS and BRAF wild type status required for anti-EGFR therapy?, Cancer Treat. Rev.
Lovly et al., 2012, Routine multiplex mutational profiling of melanomas enables enrollment in genotype-driven therapeutic trials., PLoS ONE
Falchook et al., 2013, BRAF mutant gastrointestinal stromal tumor: first report of regression with BRAF inhibitor dabrafenib (GSK2118436) and whole exomic sequencing for analysis of acquired resistance., Oncotarget
Mao et al., 2013, Resistance to BRAF inhibition in BRAF-mutant colon cancer can be overcome with PI3K inhibition or demethylating agents., Clin. Cancer Res.
Chen et al., 2014, BRAFV600E mutation and its association with clinicopathological features of colorectal cancer: a systematic review and meta-analysis., PLoS ONE
Nakayama et al., 2008, KRAS or BRAF mutation status is a useful predictor of sensitivity to MEK inhibition in ovarian cancer., Br. J. Cancer
Huillard et al., 2012, Cooperative interactions of BRAFV600E kinase and CDKN2A locus deficiency in pediatric malignant astrocytoma as a basis for rational therapy., Proc. Natl. Acad. Sci. U.S.A.
Peeters et al., 2013, Massively parallel tumor multigene sequencing to evaluate response to panitumumab in a randomized phase III study of metastatic colorectal cancer., Clin. Cancer Res.
Nagore et al., 2014, Prognostic value of BRAF mutations in localized cutaneous melanoma., J. Am. Acad. Dermatol.
Pratilas et al., 2008, Genetic predictors of MEK dependence in non-small cell lung cancer., Cancer Res.
McArthur et al., 2014, Safety and efficacy of vemurafenib in BRAF(V600E) and BRAF(V600K) mutation-positive melanoma (BRIM-3): extended follow-up of a phase 3, randomised, open-label study., Lancet Oncol.
Mao et al., 2011, BRAF V600E mutation and resistance to anti-EGFR monoclonal antibodies in patients with metastatic colorectal cancer: a meta-analysis., Mol. Biol. Rep.
De Roock et al., 2009, Clinical biomarkers in oncology: focus on colorectal cancer., Mol Diagn Ther
Haldar et al., 2011, Epidermal growth factor receptor blockers for the treatment of ovarian cancer., Cochrane Database Syst Rev
Penna et al., 2016, Primary cross-resistance to BRAFV600E-, MEK1/2- and PI3K/mTOR-specific inhibitors in BRAF-mutant melanoma cells counteracted by dual pathway blockade., Oncotarget
Corcoran et al., 2012, EGFR-mediated re-activation of MAPK signaling contributes to insensitivity of BRAF mutant colorectal cancers to RAF inhibition with vemurafenib., Cancer Discov
Xing et al., 2014, BRAF V600E and TERT promoter mutations cooperatively identify the most aggressive papillary thyroid cancer with highest recurrence., J. Clin. Oncol.
Tejpar et al., 2010, Prognostic and predictive biomarkers in resected colon cancer: current status and future perspectives for integrating genomics into biomarker discovery., Oncologist
Faber et al., 2014, mTOR inhibition specifically sensitizes colorectal cancers with KRAS or BRAF mutations to BCL-2/BCL-XL inhibition by suppressing MCL-1., Cancer Discov
Agaimy et al., 2009, V600E BRAF mutations are alternative early molecular events in a subset of KIT/PDGFRA wild-type gastrointestinal stromal tumours., J. Clin. Pathol.
De Roock et al., 2010, Effects of KRAS, BRAF, NRAS, and PIK3CA mutations on the efficacy of cetuximab plus chemotherapy in chemotherapy-refractory metastatic colorectal cancer: a retrospective consortium analysis., Lancet Oncol.
Kloos et al., 2009, Phase II trial of sorafenib in metastatic thyroid cancer., J. Clin. Oncol.
Ponti et al., 2012, Overwhelming response to Dabrafenib in a patient with double BRAF mutation (V600E; V600M) metastatic malignant melanoma., J Hematol Oncol
Paraiso et al., 2012, The HSP90 inhibitor XL888 overcomes BRAF inhibitor resistance mediated through diverse mechanisms., Clin. Cancer Res.
Kirkwood et al., 2012, Phase II, open-label, randomized trial of the MEK1/2 inhibitor selumetinib as monotherapy versus temozolomide in patients with advanced melanoma., Clin. Cancer Res.
Cardarella et al., 2013, Clinical, pathologic, and biologic features associated with BRAF mutations in non-small cell lung cancer., Clin. Cancer Res.
Nissan et al., 2014, Loss of NF1 in cutaneous melanoma is associated with RAS activation and MEK dependence., Cancer Res.
Jalili et al., 2012, Dual suppression of the cyclin-dependent kinase inhibitors CDKN2C and CDKN1A in human melanoma., J. Natl. Cancer Inst.
Gandhi et al., 2009, Alterations in genes of the EGFR signaling pathway and their relationship to EGFR tyrosine kinase inhibitor sensitivity in lung cancer cell lines., PLoS ONE
Rudin et al., 2013, Molecular characterization of acquired resistance to the BRAF inhibitor dabrafenib in a patient with BRAF-mutant non-small-cell lung cancer., J Thorac Oncol
Hauschild et al., 2012, Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial., Lancet
Prahallad et al., 2012, Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR., Nature
Boulalas et al., Mutational analysis of the BRAF gene in transitional cell carcinoma of the bladder., Int. J. Biol. Markers
Sarker et al., 2015, First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors., Clin. Cancer Res.
Crescenzi et al., 2014, Immunohistochemistry for BRAF(V600E) antibody VE1 performed in core needle biopsy samples identifies mutated papillary thyroid cancers., Horm. Metab. Res.
Andrulis et al., 2013, Targeting the BRAF V600E mutation in multiple myeloma., Cancer Discov
Rubinstein et al., 2010, Incidence of the V600K mutation among melanoma patients with BRAF mutations, and potential therapeutic response to the specific BRAF inhibitor PLX4032., J Transl Med
Kim et al., 2013, Clinical responses to vemurafenib in patients with metastatic papillary thyroid cancer harboring BRAF(V600E) mutation., Thyroid
Dienstmann et al., 2011, BRAF as a target for cancer therapy., Anticancer Agents Med Chem
Chapman et al., 2011, Improved survival with vemurafenib in melanoma with BRAF V600E mutation., N. Engl. J. Med.
Tol et al., 2010, Markers for EGFR pathway activation as predictor of outcome in metastatic colorectal cancer patients treated with or without cetuximab., Eur. J. Cancer
Ji et al., 2013, Vemurafenib synergizes with nutlin-3 to deplete survivin and suppresses melanoma viability and tumor growth., Clin. Cancer Res.
Morris et al., 2013, Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors., Cancer Discov
Sen et al., 2012, Kinase-impaired BRAF mutations in lung cancer confer sensitivity to dasatinib., Sci Transl Med
Patel et al., 2013, Clinical responses to selumetinib (AZD6244; ARRY-142886)-based combination therapy stratified by gene mutations in patients with metastatic melanoma., Cancer
He et al., 2014, Prognostic value of the BRAF V600E mutation in papillary thyroid carcinoma., Oncol Lett
Lam et al., 2010, Phase II clinical trial of sorafenib in metastatic medullary thyroid cancer., J. Clin. Oncol.
Di Nicolantonio et al., 2008, Wild-type BRAF is required for response to panitumumab or cetuximab in metastatic colorectal cancer., J. Clin. Oncol.
Zecchin et al., 2013, BRAF V600E is a determinant of sensitivity to proteasome inhibitors., Mol. Cancer Ther.
Hayes et al., 2012, Phase II efficacy and pharmacogenomic study of Selumetinib (AZD6244; ARRY-142886) in iodine-131 refractory papillary thyroid carcinoma with or without follicular elements., Clin. Cancer Res.
Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
Meckbach et al., 2014, BRAF-V600 mutations have no prognostic impact in stage IV melanoma patients treated with monochemotherapy., PLoS ONE
Ascierto et al., 2013, Phase II trial (BREAK-2) of the BRAF inhibitor dabrafenib (GSK2118436) in patients with metastatic melanoma., J. Clin. Oncol.
De Roock et al., 2011, KRAS, BRAF, PIK3CA, and PTEN mutations: implications for targeted therapies in metastatic colorectal cancer., Lancet Oncol.
Walczyk et al., 2014, The BRAF(V600E) mutation in papillary thyroid microcarcinoma: does the mutation have an impact on clinical outcome?, Clin. Endocrinol. (Oxf)
Howell et al., 2011, Both BRAF V600E mutation and older age (≥ 65 years) are associated with recurrent papillary thyroid cancer., Ann. Surg. Oncol.
Wan et al., 2004, Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF., Cell
Coffee et al., 2013, Concomitant BRAF and PI3K/mTOR blockade is required for effective treatment of BRAF(V600E) colorectal cancer., Clin. Cancer Res.
Kurman et al., 2011, Molecular pathogenesis and extraovarian origin of epithelial ovarian cancer--shifting the paradigm., Hum. Pathol.
Hatzivassiliou et al., 2013, Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers., Nature
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
Rowland et al., 2015, Meta-analysis of BRAF mutation as a predictive biomarker of benefit from anti-EGFR monoclonal antibody therapy for RAS wild-type metastatic colorectal cancer., Br. J. Cancer
Flaherty et al., 2010, Inhibition of mutated, activated BRAF in metastatic melanoma., N. Engl. J. Med.
Ohashi et al., 2012, Lung cancers with acquired resistance to EGFR inhibitors occasionally harbor BRAF gene mutations but lack mutations in KRAS, NRAS, or MEK1., Proc. Natl. Acad. Sci. U.S.A.
Falchook et al., 2012, Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial., Lancet
Paik et al., 2011, Clinical characteristics of patients with lung adenocarcinomas harboring BRAF mutations., J. Clin. Oncol.
Naoki et al., 2002, Missense mutations of the BRAF gene in human lung adenocarcinoma., Cancer Res.
Gautschi et al., 2012, A patient with BRAF V600E lung adenocarcinoma responding to vemurafenib., J Thorac Oncol
Davies et al., 2002, Mutations of the BRAF gene in human cancer., Nature
Sakaguchi et al., 1976, Microbiological oxidation of synthetic chalcocite and covellite by Thiobacillus ferrooxidans., Appl. Environ. Microbiol.
Silen et al., 1975, Acid-base balance in amphibian gastric mucosa., Am. J. Physiol.
Mir A et al., 2019, Giant Congenital Melanocytic Nevus Treated With Trametinib., Pediatrics
Jain P et al., 2017, Overcoming resistance to single-agent therapy for oncogenic <i>BRAF</i> gene fusions <i>via</i> combinatorial targeting of MAPK and PI3K/mTOR signaling pathways., Oncotarget
Noeparast A et al., 2016, Non-V600 BRAF mutations recurrently found in lung cancer predict sensitivity to the combination of Trametinib and Dabrafenib., Oncotarget
Dogruluk et al., 2015, Identification of Variant-Specific Functions of PIK3CA by Rapid Phenotyping of Rare Mutations., Cancer Res.
Winoto et al., 1989, A novel, inducible and T cell-specific enhancer located at the 3' end of the T cell receptor alpha locus., EMBO J.
Hayashi T et al., 2018, <i>RASA1</i> and <i>NF1</i> are Preferentially Co-Mutated and Define A Distinct Genetic Subset of Smoking-Associated Non-Small Cell Lung Carcinomas Sensitive to MEK Inhibition., Clin Cancer Res
Tricker et al., 2015, Combined EGFR/MEK Inhibition Prevents the Emergence of Resistance in EGFR-Mutant Lung Cancer., Cancer Discov
Kwong et al., 2012, Oncogenic NRAS signaling differentially regulates survival and proliferation in melanoma., Nat. Med.
Zick et al., 2017, Treatment inferred from mutations identified using massive parallel sequencing leads to clinical benefit in some heavily pretreated cancer patients., Medicine (Baltimore)
Posch et al., 2013, Combined targeting of MEK and PI3K/mTOR effector pathways is necessary to effectively inhibit NRAS mutant melanoma in vitro and in vivo., Proc. Natl. Acad. Sci. U.S.A.
Vujic et al., 2015, Metformin and trametinib have synergistic effects on cell viability and tumor growth in NRAS mutant cancer., Oncotarget
Ohashi et al., 2013, Characteristics of lung cancers harboring NRAS mutations., Clin. Cancer Res.
Bridgeman et al., 2016, Preclinical Evidence That Trametinib Enhances the Response to Antiangiogenic Tyrosine Kinase Inhibitors in Renal Cell Carcinoma., Mol. Cancer Ther.
Cheng et al., 2015, Paracrine Effect of NRG1 and HGF Drives Resistance to MEK Inhibitors in Metastatic Uveal Melanoma., Cancer Res.
Kaufman et al., 2017, A Transcriptional Signature Identifies LKB1 Functional Status as a Novel Determinant of MEK Sensitivity in Lung Adenocarcinoma., Cancer Res.
Khalili et al., 2012, Combination small molecule MEK and PI3K inhibition enhances uveal melanoma cell death in a mutant GNAQ- and GNA11-dependent manner., Clin. Cancer Res.
Wang et al., 2017, ATXN1L, CIC, and ETS Transcription Factors Modulate Sensitivity to MAPK Pathway Inhibition., Cell Rep
Smida et al., 2016, MEK inhibitors block growth of lung tumours with mutations in ataxia-telangiectasia mutated., Nat Commun
McEvoy CR et al., 2019, Profound MEK inhibitor response in a cutaneous melanoma harboring a GOLGA4-RAF1 fusion., J Clin Invest

TRAMETINIB ETV4

Interaction Score: 2.94

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28178529

Sources:
CIViC
TRAMETINIB ETV5

Interaction Score: 2.94

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28178529

Sources:
CIViC
TRAMETINIB ETV1

Interaction Score: 2.94

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28178529

Sources:
CIViC
TRAMETINIB RASA1

Interaction Score: 2.94

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29127119

Sources:
CIViC
TRAMETINIB DUSP6

Interaction Score: 2.94

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22169769

Sources:
CIViC
TRAMETINIB BRAF

Interaction Score: 2.22

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Trametinib + Dabrafenib

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
28512244 27338794 28784858 26392102 24265152 26811525 27500726 26343583 27770002 27760111 23248257 28344857 25370473 25706985 26732095 22663011 25265492 28891408 26369631 24265154 24265153 26469692 25309914 26916115 27048246 27697975 27222538 28268064 27297867 25665005 27312529 22389471 27797976 22805292 27488531 22798288 28783719 31010895 29903880 25452114 26314551 24933606 25265494 22169769 24345920 29072975 23020132 29431699 25399551 27283860 24583796 2493360 23715574 25656898 22038996 19773371 23845441 14679157 22180495 21156289 21663470 22356324 12460918 18541894 23406027 21129611 22536370 23470635 23251002 24594804 19018267 22586120 23325582 24388723 19010912 24508103 20857202 19537845 21975775 26678033 22448344 25024077 20350999 24163374 19561230 20619739 19255327 23031422 22351686 22048237 23833300 24576830 22997239 19238210 23524406 22735384 22281684 19404918 25370471 24570209 23612012 20630094 23489023 21426297 21639808 20413299 23812671 23614898 22649091 22972589 24396464 20368568 19001320 24107445 22241789 26619011 24586605 23918947 21163703 24354346 21594703 15035987 23549875 21683865 23934108 25157968 25989278 20818844 22773810 22608338 21483012 12460919 22743296 12068308 8006 2015 30792255 29156677 28947956

Sources:
ClearityFoundationBiomarkers JAX-CKB DoCM CIViC PharmGKB FDA OncoKB
TRAMETINIB DDX43

Interaction Score: 1.47

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24899684

Sources:
CIViC
TRAMETINIB NF1

Interaction Score: 1.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2524381 24576830 29127119

Sources:
ClearityFoundationBiomarkers CIViC OncoKB
TRAMETINIB ATXN1L

Interaction Score: 0.98

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28178529

Sources:
CIViC
TRAMETINIB CIC

Interaction Score: 0.98

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28178529

Sources:
CIViC
TRAMETINIB MAP2K1

Interaction Score: 0.62

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name GSK1120212

Novel drug target Novel Target

Notes

PMIDs:
23432625 26566875 26644315 25370473 22389471 26582713 24265154 28179366 24265153 27312529 25673644 25899310 24982505

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB CIViC MyCancerGenomeClinicalTrial OncoKB
TRAMETINIB NRAS

Interaction Score: 0.53

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type no benefit

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
22805292 27760111 27500726 22983396 28783719 28514312 26343583 22389471 28179366 27488531 23431193 25504439 25452114 23515407

Sources:
JAX-CKB CIViC PharmGKB
TRAMETINIB GNA11

Interaction Score: 0.37

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type uveal melanoma

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
22733540

Sources:
JAX-CKB
TRAMETINIB STAG2

Interaction Score: 0.37

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type decreased response

Approval Status Preclinical - Cell culture

PMIDs:
27500726

Sources:
JAX-CKB
TRAMETINIB ARAF

Interaction Score: 0.37

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24569458

Sources:
CIViC
TRAMETINIB MAP2K5

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
TRAMETINIB CDKN2A

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Palbociclib + Trametinib

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
26343583 27488531 22983396

Sources:
JAX-CKB
TRAMETINIB HRAS

Interaction Score: 0.27

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Sirolimus + Trametinib

Indication/Tumor Type head and neck squamous cell carcinoma

Response Type sensitive

PMIDs:
28783719 26343583 27222538 26882569

Sources:
JAX-CKB PharmGKB
TRAMETINIB MAP2K2

Interaction Score: 0.26

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
23432625 25452114

Sources:
TALC MyCancerGenome ClearityFoundationClinicalTrial CIViC MyCancerGenomeClinicalTrial
TRAMETINIB KRAS

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Pazopanib + Trametinib

Indication/Tumor Type thyroid cancer

combination therapy Dasatinib + Trametinib

PMIDs:
27876675 24685132 22169769 24915778 26324075 27222538 26582713 26882569 28179366 25665005 22805291 27556948 27659046 26343583 27338794 27312529 26369631 26644315

Sources:
ClearityFoundationBiomarkers JAX-CKB CIViC PharmGKB OncoKB
TRAMETINIB MAP2K7

Interaction Score: 0.25

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
TRAMETINIB MAP2K4

Interaction Score: 0.25

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
TRAMETINIB MAP2K6

Interaction Score: 0.25

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
TRAMETINIB MAP2K3

Interaction Score: 0.25

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
TRAMETINIB GNAQ

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GSK2126458 + Trametinib

Indication/Tumor Type uveal melanoma

Response Type sensitive

PMIDs:
22733540

Sources:
JAX-CKB
TRAMETINIB VHL

Interaction Score: 0.2

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Sunitinib + Trametinib

Indication/Tumor Type kidney cancer

Response Type predicted – sensitive

PMIDs:
26487278

Sources:
JAX-CKB
TRAMETINIB CTNNB1

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type liver cancer

Response Type resistant

Approval Status Preclinical

PMIDs:
26343583

Sources:
JAX-CKB
TRAMETINIB RAF1

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30835257

Sources:
CIViC
TRAMETINIB RB1

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type decreased response

PMIDs:
27488531

Sources:
JAX-CKB
TRAMETINIB STK11

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
27821489

Sources:
JAX-CKB
TRAMETINIB ERBB3

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25952648

Sources:
CIViC
TRAMETINIB PIK3CA

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Palbociclib + Trametinib

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
26882569 27797976 26469692 27659046 26627007 26369631

Sources:
JAX-CKB
TRAMETINIB FGFR2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type no benefit

PMIDs:
27338794

Sources:
JAX-CKB
TRAMETINIB MET

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy INC280 + Trametinib

Indication/Tumor Type collecting duct carcinoma

Response Type sensitive

PMIDs:
28783719 25952648

Sources:
JAX-CKB CIViC
TRAMETINIB ATM

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27922010

Sources:
CIViC
TRAMETINIB SRC

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type thyroid cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
27222538

Sources:
JAX-CKB
TRAMETINIB KIT

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Clinical Study

Response Type no benefit

PMIDs:
28514312

Sources:
JAX-CKB
TRAMETINIB FGFR3

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type lung cancer

Response Type no benefit

Approval Status Preclinical

PMIDs:
27338794

Sources:
JAX-CKB
TRAMETINIB EGFR

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Cell line xenograft

Indication/Tumor Type collecting duct carcinoma

Approval Status Preclinical - Pdx

PMIDs:
28783719 27312529 26582713 26036643

Sources:
JAX-CKB
TRAMETINIB G6PD

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
TRAMETINIB FGFR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type lung cancer

Response Type no benefit

Approval Status Preclinical

PMIDs:
27338794

Sources:
JAX-CKB
TRAMETINIB TP53

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy ABT-263 + Alpelisib + Erlotinib + Trametinib

Evidence Type Actionable

Approval Status Preclinical - Cell culture

PMIDs:
27659046

Sources:
JAX-CKB

MyCancerGenome: TRAMETINIB
- Version: 20-Jun-2017
Alternate Names:

GSK1120212 Development Name

TRAMETINIB Generic Name

Drug Info:

Drug Class Kinase Inhibitors

Notes allosteric inhibitor

FDA Approval Melanoma (with BRAF V600 mutation)

Publications:
TdgClinicalTrial: TRAMETINIB
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:

DoCM: TRAMETINIB

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Flaherty et al., 2012, Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations., N. Engl. J. Med.

Falchook et al., 2012, Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial., Lancet

Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.

JAX-CKB: GSK1120212
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:

Gandara et al., 2017, A Phase 1/1b Study Evaluating Trametinib Plus Docetaxel or Pemetrexed in Patients With Advanced Non-Small Cell Lung Cancer., J Thorac Oncol

JAX-CKB: Trametinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.

Yao et al., 2017, Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS., Nature

Tricker et al., 2015, Combined EGFR/MEK Inhibition Prevents the Emergence of Resistance in EGFR-Mutant Lung Cancer., Cancer Discov

CIViC: TRAMETINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Imielinski et al., 2014, Oncogenic and sorafenib-sensitive ARAF mutations in lung adenocarcinoma., J. Clin. Invest.

Russo et al., 2016, Tumor Heterogeneity and Lesion-Specific Response to Targeted Therapy in Colorectal Cancer., Cancer Discov

Sun et al., 2014, Intrinsic resistance to MEK inhibition in KRAS mutant lung and colon cancer through transcriptional induction of ERBB3., Cell Rep

TALC: TRAMETINIB
- Version: 12-May-2016
Alternate Names:

TRAMETINIB Primary Drug Name

TRAMETINIB Drug Generic Name

GSK1120212 Drug Synonym

Drug Info:

Publications:
TTD: Trametinib
- Version: 2020.06.01
Alternate Names:

D04XVN TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL2103875
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: TRAMETINIB
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
OncoKB: Trametinib
- Version: 23-July-2020
Alternate Names:

Drug Info:

Publications:
ClearityFoundationClinicalTrial: TRAMETINIB
- Version: 15-June-2013
Alternate Names:

Drug Info:

Publications:
ClearityFoundationBiomarkers: TRAMETINIB
- Version: 26-July-2013
Alternate Names:

Drug Info:

Publications:
PharmGKB: trametinib
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:
FDA: Trametinib
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:

combination therapy	Trametinib + Dabrafenib
Indication/Tumor Type	colorectal cancer
Response Type	sensitive

Response Type	no benefit
Indication/Tumor Type	melanoma
Response Type	sensitive

Indication/Tumor Type	uveal melanoma
Response Type	sensitive
Approval Status	Preclinical - Cell culture

combination therapy	Palbociclib + Trametinib
Indication/Tumor Type	melanoma
Response Type	sensitive

combination therapy	Sirolimus + Trametinib
Indication/Tumor Type	head and neck squamous cell carcinoma
Response Type	sensitive

combination therapy	Pazopanib + Trametinib
Indication/Tumor Type	thyroid cancer
combination therapy	Dasatinib + Trametinib

combination therapy	GSK2126458 + Trametinib
Indication/Tumor Type	uveal melanoma
Response Type	sensitive

combination therapy	Sunitinib + Trametinib
Indication/Tumor Type	kidney cancer
Response Type	predicted – sensitive

Indication/Tumor Type	liver cancer
Response Type	resistant
Approval Status	Preclinical

Evidence Type	Actionable
Approval Status	Preclinical - Cell culture
Response Type	decreased response

antagonist (inhibitory)
inhibitor (inhibitory)

antagonist (inhibitory)
inhibitor (inhibitory)

Indication/Tumor Type	non-small cell lung carcinoma
Response Type	sensitive
Approval Status	Preclinical - Cell culture

combination therapy	INC280 + Trametinib
Indication/Tumor Type	collecting duct carcinoma
Response Type	sensitive

Indication/Tumor Type	lung cancer
Response Type	no benefit
Approval Status	Preclinical

Approval Status	Preclinical - Cell line xenograft
Indication/Tumor Type	collecting duct carcinoma
Approval Status	Preclinical - Pdx

combination therapy	ABT-263 + Alpelisib + Erlotinib + Trametinib
Evidence Type	Actionable
Approval Status	Preclinical - Cell culture

TRAMETINIB	Primary Drug Name
TRAMETINIB	Drug Generic Name
GSK1120212	Drug Synonym

TRAMETINIB Drug Record

TRAMETINIB chembl:CHEMBL2103875 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28178529

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28178529

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28178529

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29127119

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22169769

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Trametinib + Dabrafenib Indication/Tumor Type colorectal cancer Response Type sensitive

Sources: ClearityFoundationBiomarkers JAX-CKB DoCM CIViC PharmGKB FDA OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24899684

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 2524381 24576830 29127119

Sources: ClearityFoundationBiomarkers CIViC OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28178529

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28178529

Sources: CIViC

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: Trial Name GSK1120212 Novel drug target Novel Target Notes

PMIDs: 23432625 26566875 26644315 25370473 22389471 26582713 24265154 28179366 24265153 27312529 25673644 25899310 24982505

Sources: TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB CIViC MyCancerGenomeClinicalTrial OncoKB

Interaction Types & Directionality: n/a

Interaction Info: Response Type no benefit Indication/Tumor Type melanoma Response Type sensitive

PMIDs: 22805292 27760111 27500726 22983396 28783719 28514312 26343583 22389471 28179366 27488531 23431193 25504439 25452114 23515407

Sources: JAX-CKB CIViC PharmGKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type uveal melanoma Response Type sensitive Approval Status Preclinical - Cell culture

PMIDs: 22733540

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type melanoma Response Type decreased response Approval Status Preclinical - Cell culture

PMIDs: 27500726

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24569458

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Palbociclib + Trametinib Indication/Tumor Type melanoma Response Type sensitive

PMIDs: 26343583 27488531 22983396

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Sirolimus + Trametinib Indication/Tumor Type head and neck squamous cell carcinoma Response Type sensitive

PMIDs: 28783719 26343583 27222538 26882569

Sources: JAX-CKB PharmGKB

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: Notes

PMIDs: 23432625 25452114

Sources: TALC MyCancerGenome ClearityFoundationClinicalTrial CIViC MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
28178529

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
28178529

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
28178529

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
29127119

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
22169769

Sources:
CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Trametinib + Dabrafenib

Indication/Tumor Type colorectal cancer

Response Type sensitive

Sources:
ClearityFoundationBiomarkers JAX-CKB DoCM CIViC PharmGKB FDA OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
24899684

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
2524381 24576830 29127119

Sources:
ClearityFoundationBiomarkers CIViC OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
28178529

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
28178529

Sources:
CIViC

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name GSK1120212

Novel drug target Novel Target

Notes

PMIDs:
23432625 26566875 26644315 25370473 22389471 26582713 24265154 28179366 24265153 27312529 25673644 25899310 24982505

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB CIViC MyCancerGenomeClinicalTrial OncoKB

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type no benefit

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
22805292 27760111 27500726 22983396 28783719 28514312 26343583 22389471 28179366 27488531 23431193 25504439 25452114 23515407

Sources:
JAX-CKB CIViC PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type uveal melanoma

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
22733540

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type decreased response

Approval Status Preclinical - Cell culture

PMIDs:
27500726

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
24569458

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Palbociclib + Trametinib

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
26343583 27488531 22983396

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Sirolimus + Trametinib

Indication/Tumor Type head and neck squamous cell carcinoma

Response Type sensitive

PMIDs:
28783719 26343583 27222538 26882569

Sources:
JAX-CKB PharmGKB

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
23432625 25452114

Sources:
TALC MyCancerGenome ClearityFoundationClinicalTrial CIViC MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Pazopanib + Trametinib

Indication/Tumor Type thyroid cancer

combination therapy Dasatinib + Trametinib

PMIDs:
27876675 24685132 22169769 24915778 26324075 27222538 26582713 26882569 28179366 25665005 22805291 27556948 27659046 26343583 27338794 27312529 26369631 26644315

Sources:
ClearityFoundationBiomarkers JAX-CKB CIViC PharmGKB OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial