DGIdb - PEMETREXED Drug Record

PEMETREXED chembl:CHEMBL225072 ApprovedAntineoplasticImmunotherapy

Alternate Names:

NSC-698037
ALIMTA
LY-231514
LY231514
PEMETREXED
LY-2315
ALIMTA®
pubchem.compound:446556
rxcui:68446
chemidplus:137281-23-3
drugbank:00642
chembl:CHEMBL225072

Drug Info:

FDA Approval	2004
Drug Class	small molecule
Drug Indications	Antineoplastic Agents
FDA Approval	not approved
Drug Class	Small molecule
Drug Indications	antineoplastic agent
Drug Class	antineoplastic agents
Year of Approval	2004

(7 More Sources)

Publications:

Pivot et al., 2001, Pemetrexed disodium in recurrent locally advanced or metastatic squamous cell carcinoma of the head and neck., Br. J. Cancer
Kindler, 2002, Pemetrexed in pancreatic cancer., Semin. Oncol.
Hanauske et al., 2001, Pemetrexed disodium: a novel antifolate clinically active against multiple solid tumors., Oncologist
Mauritz et al., 2002, Multiple mechanisms of resistance to methotrexate and novel antifolates in human CCRF-CEM leukemia cells and their implications for folate homeostasis., Biochem. Pharmacol.
Adjei, 2001, Gemcitabine and Pemetrexed disodium in treating breast cancer., Oncology (Williston Park, N.Y.)
Adjei, 2002, Pemetrexed in the treatment of selected solid tumors., Semin. Oncol.
Giovannetti et al., 2005, Cellular and pharmacogenetics foundation of synergistic interaction of pemetrexed and gemcitabine in human non-small-cell lung cancer cells., Mol. Pharmacol.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Norman, 2001, Pemetrexed disodium (Eli Lilly)., Curr Opin Investig Drugs
Schultz et al., Sequence dependence of Alimta (LY231514, MTA) combined with doxorubicin in ZR-75-1 human breast carcinoma cells., Anticancer Res.
Molina et al., 2003, The role of Pemetrexed (Alimta , LY231514) in lung cancer therapy., Clin Lung Cancer
Adjei, 2001, Gemcitabine and pemetrexed disodium combinations in vitro and in vivo., Lung Cancer
Corrigan A et al., 2014, Pharmacogenetics of pemetrexed combination therapy in lung cancer: pathway analysis reveals novel toxicity associations., Pharmacogenomics J
Jung M et al., 2013, Pharmacogenomic assessment of outcomes of pemetrexed-treated patients with adenocarcinoma of the lung., Yonsei Med J
Chen et al., 2011, Thymidylate synthase and dihydrofolate reductase expression in non-small cell lung carcinoma: the association with treatment efficacy of pemetrexed., Lung Cancer
Kasai et al., 2013, Thymidylate synthase gene copy number as a predictive marker for response to pemetrexed treatment of lung adenocarcinoma., Anticancer Res.
Shimizu et al., 2012, Association between expression of thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase and efficacy of pemetrexed in advanced non-small cell lung cancer., Anticancer Res.
Chamizo et al., 2015, Thymidylate synthase expression as a predictive biomarker of pemetrexed sensitivity in advanced non-small cell lung cancer., BMC Pulm Med
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
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
Pérez-Ramírez C et al., 2019, Pharmacogenetics of platinum-based chemotherapy: impact of DNA repair and folate metabolism gene polymorphisms on prognosis of non-small cell lung cancer patients., Pharmacogenomics J
Chen JS et al., 2010, A phase I/II and pharmacogenomic study of pemetrexed and cisplatin in patients with unresectable, advanced gastric carcinoma., Anticancer Drugs
Smit EF et al., 2009, Randomized phase II and pharmacogenetic study of pemetrexed compared with pemetrexed plus carboplatin in pretreated patients with advanced non-small-cell lung cancer., J Clin Oncol
Li et al., 2014, Response to pemetrexed rechallenge after acquired resistance of EGFR-TKI in a patient with advanced NSCLC., Lung Cancer
Yang JC et al., 2020, A Randomized Phase 2 Study of Gefitinib With or Without Pemetrexed as First-line Treatment in Nonsquamous NSCLC With EGFR Mutation: Final Overall Survival and Biomarker Analysis., J Thorac Oncol
Wang L et al., 2011, Synthesis, biological, and antitumor activity of a highly potent 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitor with proton-coupled folate transporter and folate receptor selectivity over the reduced folate carrier that inhibits β-glycinamide ribonucleotide formyltransferase., J Med Chem
Adjei AA et al., 2010, Phase II trial of pemetrexed plus bevacizumab for second-line therapy of patients with advanced non-small-cell lung cancer: NCCTG and SWOG study N0426., J Clin Oncol
Goldman ID et al., 2002, Molecular, biochemical, and cellular pharmacology of pemetrexed., Semin Oncol
Poklepovic et al., 2016, Phase I study of pemetrexed with sorafenib in advanced solid tumors., Oncotarget
Wang L et al., 2015, 6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptor α and the Proton-Coupled Folate Transporter in Human Tumors., J Med Chem
Mitchell-Ryan S et al., 2013, Discovery of 5-substituted pyrrolo[2,3-d]pyrimidine antifolates as dual-acting inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis: implications of inhibiting 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase to ampk activation and antitumor activity., J Med Chem
Racanelli et al., 2009, Therapeutics by cytotoxic metabolite accumulation: pemetrexed causes ZMP accumulation, AMPK activation, and mammalian target of rapamycin inhibition., Cancer Res.
Lee et al., 2011, Anaplastic lymphoma kinase translocation: a predictive biomarker of pemetrexed in patients with non-small cell lung cancer., J Thorac Oncol

PEMETREXED GART

Interaction Score: 17.67

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Trial Name Alimta

PMIDs:
11531245 12571811 11524555 10592235 11252887 12023793 15795320 11848474 11742712 14596699

Sources:
TdgClinicalTrial TEND
PEMETREXED ATIC

Interaction Score: 11.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
24256410 12571811 11524555 19549896

Sources:
DTC
PEMETREXED FOLR3

Interaction Score: 8.83

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24732178

Sources:
PharmGKB
PEMETREXED SLC46A1

Interaction Score: 6.62

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21879757 26317331

Sources:
DTC
PEMETREXED DHFR

Interaction Score: 5.3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Alimta

Novel drug target Established target

Trial Name -

PMIDs:
11531245 12571811 11524555 11841783 11252887 12023793 15795320 11752352 11763166 11848474 14596699 11742712 24732178 23709418

Sources:
TdgClinicalTrial ClearityFoundationClinicalTrial TEND PharmGKB
PEMETREXED SLC19A1

Interaction Score: 2.41

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21879757 24732178 19841321 12571805

Sources:
DTC PharmGKB
PEMETREXED TYMS

Interaction Score: 2.27

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Alimta

Novel drug target Established target

Trial Name -

PMIDs:
21367480 23645741 23060591 26502926 11531245 12571811 11524555 11252887 12023793 15795320 11752352 11763166 11848474 14596699 11742712

Sources:
ClearityFoundationBiomarkers TdgClinicalTrial TEND CIViC
PEMETREXED GGH

Interaction Score: 1.77

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24732178

Sources:
PharmGKB
PEMETREXED MTHFR

Interaction Score: 0.88

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29662106 24732178 20634689 19307503

Sources:
PharmGKB
PEMETREXED ALK

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21642865

Sources:
CIViC
PEMETREXED KRAS

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Pemetrexed + GSK1120212

Indication/Tumor Type non-small cell lung carcinoma

Response Type predicted – sensitive

PMIDs:
27876675

Sources:
JAX-CKB CIViC
PEMETREXED PTEN

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Pemetrexed + Sorafenib

Indication/Tumor Type Advanced Solid Tumor

Response Type predicted – sensitive

PMIDs:
27213589

Sources:
JAX-CKB
PEMETREXED ABCC2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
PEMETREXED EGFR

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24636847 31605797

Sources:
CIViC

TEND: PEMETREXED
- Version: 01-August-2011
Alternate Names:

PEMETREXED Primary Drug Name

Drug Info:

Year of Approval 2004

Drug Class antineoplastic agents

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

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:

DTC: PEMETREXED

Version: 02-September-2020

Alternate Names:

CHEMBL225072 ChEMBL Drug ID

Drug Info:

Publications:

Wang L et al., 2011, Synthesis, biological, and antitumor activity of a highly potent 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitor with proton-coupled folate transporter and folate receptor selectivity over the reduced folate carrier that inhibits β-glycinamide ribonucleotide formyltransferase., J Med Chem

Wang L et al., 2015, 6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptor α and the Proton-Coupled Folate Transporter in Human Tumors., J Med Chem

Mitchell-Ryan S et al., 2013, Discovery of 5-substituted pyrrolo[2,3-d]pyrimidine antifolates as dual-acting inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis: implications of inhibiting 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase to ampk activation and antitumor activity., J Med Chem

JAX-CKB: Pemetrexed

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

Poklepovic et al., 2016, Phase I study of pemetrexed with sorafenib in advanced solid tumors., Oncotarget

PharmGKB: pemetrexed

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Corrigan A et al., 2014, Pharmacogenetics of pemetrexed combination therapy in lung cancer: pathway analysis reveals novel toxicity associations., Pharmacogenomics J

Adjei AA et al., 2010, Phase II trial of pemetrexed plus bevacizumab for second-line therapy of patients with advanced non-small-cell lung cancer: NCCTG and SWOG study N0426., J Clin Oncol

Goldman ID et al., 2002, Molecular, biochemical, and cellular pharmacology of pemetrexed., Semin Oncol

CIViC: PEMETREXED

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Yang JC et al., 2020, A Randomized Phase 2 Study of Gefitinib With or Without Pemetrexed as First-line Treatment in Nonsquamous NSCLC With EGFR Mutation: Final Overall Survival and Biomarker Analysis., J Thorac Oncol

Li et al., 2014, Response to pemetrexed rechallenge after acquired resistance of EGFR-TKI in a patient with advanced NSCLC., Lung Cancer

Kasai et al., 2013, Thymidylate synthase gene copy number as a predictive marker for response to pemetrexed treatment of lung adenocarcinoma., Anticancer Res.

TTD: Pemetrexed
- Version: 2020.06.01
Alternate Names:

D0Y4GO TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL225072
- Version: ChEMBL_27
Alternate Names:

Drug Info:

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

Drug Info:

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

Drug Info:

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

Drug Info:

Publications:

Trial Name	-
Novel drug target	Established target
Trial Name	Alimta

combination therapy	Pemetrexed + GSK1120212
Indication/Tumor Type	non-small cell lung carcinoma
Response Type	predicted – sensitive

combination therapy	Pemetrexed + Sorafenib
Indication/Tumor Type	Advanced Solid Tumor
Response Type	predicted – sensitive

PEMETREXED Drug Record

PEMETREXED chembl:CHEMBL225072 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target Trial Name Alimta

PMIDs: 11531245 12571811 11524555 10592235 11252887 12023793 15795320 11848474 11742712 14596699

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 24256410 12571811 11524555 19549896

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24732178

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21879757 26317331

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Alimta Novel drug target Established target Trial Name -

PMIDs: 11531245 12571811 11524555 11841783 11252887 12023793 15795320 11752352 11763166 11848474 14596699 11742712 24732178 23709418

Sources: TdgClinicalTrial ClearityFoundationClinicalTrial TEND PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21879757 24732178 19841321 12571805

Sources: DTC PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Alimta Novel drug target Established target Trial Name -

PMIDs: 21367480 23645741 23060591 26502926 11531245 12571811 11524555 11252887 12023793 15795320 11752352 11763166 11848474 14596699 11742712

Sources: ClearityFoundationBiomarkers TdgClinicalTrial TEND CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24732178

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29662106 24732178 20634689 19307503

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21642865

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Pemetrexed + GSK1120212 Indication/Tumor Type non-small cell lung carcinoma Response Type predicted – sensitive

PMIDs: 27876675

Sources: JAX-CKB CIViC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Pemetrexed + Sorafenib Indication/Tumor Type Advanced Solid Tumor Response Type predicted – sensitive

PMIDs: 27213589

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24636847 31605797

Sources: CIViC

TEND: PEMETREXED

Alternate Names: PEMETREXED Primary Drug Name

Drug Info: Year of Approval 2004 Drug Class antineoplastic agents

Publications:

TdgClinicalTrial: PEMETREXED

Alternate Names:

Drug Info: Drug Indications antineoplastic agent Drug Class Small molecule FDA Approval not approved

Publications:

DTC: PEMETREXED

Alternate Names: CHEMBL225072 ChEMBL Drug ID

Drug Info:

JAX-CKB: Pemetrexed

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 Poklepovic et al., 2016, Phase I study of pemetrexed with sorafenib in advanced solid tumors., Oncotarget

PharmGKB: pemetrexed

Alternate Names:

Drug Info:

CIViC: PEMETREXED

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Trial Name Alimta

PMIDs:
11531245 12571811 11524555 10592235 11252887 12023793 15795320 11848474 11742712 14596699

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
24256410 12571811 11524555 19549896

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
24732178

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
21879757 26317331

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Alimta

Novel drug target Established target

Trial Name -

PMIDs:
11531245 12571811 11524555 11841783 11252887 12023793 15795320 11752352 11763166 11848474 14596699 11742712 24732178 23709418

Sources:
TdgClinicalTrial ClearityFoundationClinicalTrial TEND PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
21879757 24732178 19841321 12571805

Sources:
DTC PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Alimta

Novel drug target Established target

Trial Name -

PMIDs:
21367480 23645741 23060591 26502926 11531245 12571811 11524555 11252887 12023793 15795320 11752352 11763166 11848474 14596699 11742712

Sources:
ClearityFoundationBiomarkers TdgClinicalTrial TEND CIViC

Interaction Types & Directionality:

n/a

PMIDs:
24732178

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
29662106 24732178 20634689 19307503

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
21642865

Sources:
CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Pemetrexed + GSK1120212

Indication/Tumor Type non-small cell lung carcinoma

Response Type predicted – sensitive

PMIDs:
27876675

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Pemetrexed + Sorafenib

Indication/Tumor Type Advanced Solid Tumor

Response Type predicted – sensitive

PMIDs:
27213589

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
24636847 31605797

Sources:
CIViC

Alternate Names:

PEMETREXED Primary Drug Name

Drug Info:

Year of Approval 2004

Drug Class antineoplastic agents

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Alternate Names:

CHEMBL225072 ChEMBL Drug ID

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

Poklepovic et al., 2016, Phase I study of pemetrexed with sorafenib in advanced solid tumors., Oncotarget

Alternate Names:

D0Y4GO TTD Drug ID