Pemetrexed
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Also known as AlimtaLY-231514LY231514NSC-698037PemfexySID124893263SID50112739SID525786[3H]-PemetrexedPemetrexate
Summary
Pemetrexed (CHEMBL225072) is an approved small-molecule antineoplastic agent (ATC L01BA04) targeting DHFR, GART, and TYMS; indicated across 64 conditions including neoplasm and mesothelioma; with CIViC clinical evidence for 13 variant-indication associations (e.g. EGFR L858R OR EGFR Exon 19 Deletion in lung non-small cell carcinoma).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01BA04
- Targets: 3 (DHFR, GART, TYMS)
- Indications: 64 conditions
- Clinical trials: 890
- Precision-oncology evidence (CIViC): 13 variant–indication associations
- Chemistry: 427.4 Da · C20H21N5O6
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL225072 |
| Name | Pemetrexed |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 135410875 |
| ChEBI | CHEBI:63616 |
| ATC | L01BA04 |
| Molecular formula | C20H21N5O6 |
| Molecular weight | 427.4 |
| InChIKey | WBXPDJSOTKVWSJ-ZDUSSCGKSA-N |
SMILES: C1=CC(=CC=C1CCC2=CNC3=C2C(=O)NC(=N3)N)C(=O)N[C@@H](CCC(=O)O)C(=O)O
IUPAC name: (2S)-2-[[4-[2-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]amino]pentanedioic acid
ChEBI definition: An N-acylglutamic acid in which the N-acyl group is specified as 4-[2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl. Inhibits thymidylate synthase (TS), 421 dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT).
Pharmacological roles (ChEBI): antineoplastic agent, EC 2.1.1.45 (thymidylate synthase) inhibitor, EC 1.5.1.3 (dihydrofolate reductase) inhibitor, EC 2.1.2.2 (phosphoribosylglycinamide formyltransferase) inhibitor.
Other ChEBI roles (chemical / environmental): antimetabolite.
Also known as: Alimta, LY-231514, LY231514, NSC-698037, Pemetrexed, Pemfexy, pemetrexed, SID124893263, SID50112739, SID525786, PEMETREXED, [3H]-Pemetrexed
Parent form; salt/anhydrous children: CHEMBL2360464, CHEMBL3989962, CHEMBL5315053, CHEMBL6068329, CHEMBL6068335
Patent coverage: 14,919 distinct patent families (55,761 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 55,151 (99%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| DHFR | dihydrofolate reductase | Inhibition | 8.15 | 69.8% | P00374 |
| GART | phosphoribosylglycinamide formyltransferase, phosphoribosylglycinamide synthetase, phosphoribosylaminoimidazole synthetase | Inhibition | 5.03 | 32.4% | P22102 |
| TYMS | thymidylate synthetase | Inhibition | 6.96 | 50.8% | P04818 |
Broader ChEMBL bioactivity targets: 19 (assay-derived). Sample: Serine hydroxymethyltransferase, cytosolic, Proton-coupled folate transporter, Dihydrofolate reductase, Thymidylate synthase, Dihydrofolate reductase, Folate receptor alpha, Bifunctional dihydrofolate reductase-thymidylate synthase, Bifunctional purine biosynthesis protein ATIC, Thymidylate synthase, Dihydrofolate reductase.
Bioactivity
ChEMBL activities: 98 potent at pChembl ≥ 5 of 115 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| TYMS | 8.89 | Ki | 1.3 | nM | CHEMBL_ACT_24862080 |
| TYMS | 8.89 | Ki | 1.3 | nM | CHEMBL_ACT_3465181 |
| DHFR | 8.15 | Ki | 7 | nM | CHEMBL_ACT_1495527 |
| DHFR | 8.14 | Ki | 7.2 | nM | CHEMBL_ACT_24862081 |
| DHFR | 8.14 | Ki | 7.2 | nM | CHEMBL_ACT_3465182 |
| SLC46A1 | 8.08 | IC50 | 8.3 | nM | CHEMBL_ACT_18863169 |
| GART | 7.93 | IC50 | 11.74 | nM | CHEMBL_ACT_15200056 |
| SLC46A1 | 7.88 | IC50 | 13.2 | nM | CHEMBL_ACT_15067597 |
| SLC46A1 | 7.88 | IC50 | 13.2 | nM | CHEMBL_ACT_15200019 |
| SLC46A1 | 7.88 | IC50 | 13.2 | nM | CHEMBL_ACT_18527797 |
| SLC19A1 | 7.62 | IC50 | 23.8 | nM | CHEMBL_ACT_18863181 |
| SLC19A1 | 7.58 | IC50 | 26.2 | nM | CHEMBL_ACT_18863118 |
| GART | 7.54 | IC50 | 29.2 | nM | CHEMBL_ACT_18863348 |
| GART | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_2228903 |
| GART | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_2527328 |
| FOLR1 | 7.38 | IC50 | 42 | nM | CHEMBL_ACT_15072119 |
| FOLR1 | 7.38 | IC50 | 42 | nM | CHEMBL_ACT_15200011 |
| FOLR1 | 7.38 | IC50 | 42 | nM | CHEMBL_ACT_18527753 |
| FOLR1 | 7.38 | IC50 | 42 | nM | CHEMBL_ACT_18863143 |
| FRK | 7.38 | IC50 | 42 | nM | CHEMBL_ACT_29103813 |
| FOLR2 | 7.22 | IC50 | 60 | nM | CHEMBL_ACT_15072101 |
| FOLR2 | 7.22 | IC50 | 60 | nM | CHEMBL_ACT_18527775 |
| FOLR2 | 7.22 | IC50 | 60 | nM | CHEMBL_ACT_18863156 |
| GART | 7.19 | Ki | 65 | nM | CHEMBL_ACT_24862082 |
| SLC46A1 | 7.17 | IC50 | 66.8 | nM | CHEMBL_ACT_18863193 |
| DHFR | 7.17 | IC50 | 68 | nM | CHEMBL_ACT_20685614 |
| TYMS | 7.16 | IC50 | 70 | nM | CHEMBL_ACT_18314595 |
| SLC46A1 | 7.03 | Ki | 94 | nM | CHEMBL_ACT_12078936 |
| SLC46A1 | 7.03 | Ki | 94 | nM | CHEMBL_ACT_19443032 |
| SLC46A1 | 7.02 | Ki | 96 | nM | CHEMBL_ACT_3101242 |
Target pathways
Aggregated over 3 target gene(s): DHFR, GART, TYMS.
Top Reactome pathways
5 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| G1/S-Specific Transcription | 2 | DHFR, TYMS |
| Tetrahydrobiopterin (BH4) synthesis, recycling, salvage and regulation | 1 | DHFR |
| Metabolism of folate and pterines | 1 | DHFR |
| Interconversion of nucleotide di- and triphosphates | 1 | TYMS |
| Purine ribonucleoside monophosphate biosynthesis | 1 | GART |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| one-carbon metabolic process | 2 |
| negative regulation of translation | 2 |
| tetrahydrofolate metabolic process | 2 |
| tetrahydrobiopterin biosynthetic process | 1 |
| axon regeneration | 1 |
| response to methotrexate | 1 |
| dihydrofolate metabolic process | 1 |
| tetrahydrofolate biosynthetic process | 1 |
| folic acid metabolic process | 1 |
| regulation of removal of superoxide radicals | 1 |
| brainstem development | 1 |
| purine nucleotide biosynthetic process | 1 |
| GMP biosynthetic process | 1 |
| ‘de novo’ IMP biosynthetic process | 1 |
| purine ribonucleoside monophosphate biosynthetic process | 1 |
Indications & clinical
Indications
64 indications (5 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| mesothelioma | 4 | MONDO:0005065 | EFO:0000588 |
| malignant pleural mesothelioma | 4 | MONDO:0005112 | EFO:0000770 |
| malignant peritoneal mesothelioma | 4 | MONDO:0005512 | EFO:0005567 |
| non-small cell lung carcinoma | 3 | MONDO:0005233 | EFO:0003060 |
| gastric carcinoma | 3 | MONDO:0004950 | EFO:0000178 |
| carcinoma | 3 | MONDO:0004993 | EFO:0000313 |
| lung adenocarcinoma | 3 | MONDO:0005061 | EFO:0000571 |
| small cell lung carcinoma | 3 | MONDO:0008433 | EFO:0000702 |
| gastric neoplasm | 3 | MONDO:0021085 | EFO:0003897 |
| upper aerodigestive tract neoplasm | 3 | MONDO:0005398 | EFO:0004284 |
| head and neck cancer | 3 | MONDO:0005627 | EFO:0006859 |
| lung neoplasm | 3 | MONDO:0021117 | MONDO:0008903 |
| cervical adenocarcinoma | 3 | MONDO:0005153 | EFO:0001416 |
| head and neck squamous cell carcinoma | 2 | MONDO:0010150 | EFO:0000181 |
| adenocarcinoma | 2 | MONDO:0004970 | EFO:0000228 |
| osteosarcoma | 2 | MONDO:0009807 | EFO:0000637 |
| renal cell carcinoma | 2 | MONDO:0005086 | EFO:0000681 |
| sarcoma | 2 | MONDO:0005089 | EFO:0000691 |
| squamous cell lung carcinoma | 2 | MONDO:0005097 | EFO:0000708 |
| exocrine pancreatic carcinoma | 2 | MONDO:0005192 | EFO:0002618 |
| carcinoma of esophagus | 2 | MONDO:0019086 | EFO:0002916 |
| medulloblastoma | 2 | MONDO:0007959 | EFO:0002939 |
| breast neoplasm | 2 | MONDO:0021100 | EFO:0003869 |
| colorectal neoplasm | 2 | MONDO:0005335 | EFO:0004142 |
| nasopharyngeal neoplasm | 2 | MONDO:0005375 | EFO:0004252 |
| male breast carcinoma | 2 | MONDO:0005628 | EFO:0006861 |
| urothelial carcinoma | 2 | MONDO:0040679 | EFO:0008528 |
| rectal cancer | 2 | MONDO:0006519 | EFO:1000657 |
| neuroendocrine neoplasm | 2 | MONDO:0019496 | EFO:1001901 |
| peritoneal neoplasm | 2 | MONDO:0006901 | MONDO:0002087 |
| fallopian tube neoplasm | 2 | MONDO:0021092 | MONDO:0002158 |
| ovarian cancer | 2 | MONDO:0008170 | MONDO:0008170 |
| ovarian carcinoma | 2 | MONDO:0005140 | EFO:0001075 |
| fallopian tube carcinoma | 2 | MONDO:0006206 | EFO:1000251 |
| diffuse large B-cell lymphoma | 2 | MONDO:0018905 | EFO:0000403 |
| lung large cell carcinoma | 2 | MONDO:0003050 | EFO:0003050 |
| malignant mesothelioma | 2 | MONDO:0006292 | EFO:1000355 |
| lymphoma | 1 | MONDO:0005062 | EFO:0000574 |
| non-Hodgkin lymphoma | 1 | MONDO:0018908 | EFO:0005952 |
| thymoma | 1 | MONDO:0006456 | EFO:1000581 |
| metastatic melanoma | 1 | MONDO:0005191 | EFO:0002617 |
| chordoma | 1 | MONDO:0008978 | MONDO:0008978 |
| endometrium neoplasm | 1 | MONDO:0021251 | MONDO:0011962 |
| primary myelofibrosis | 1 | MONDO:0009692 | MONDO:0044903 |
| triple-negative breast carcinoma | 1 | MONDO:0005494 | EFO:0005537 |
| uveal melanoma | 1 | MONDO:0006486 | EFO:1000616 |
| glioma | 0 | MONDO:0021042 | MONDO:0100342 |
16 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 890.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 420 |
| PHASE3 | 188 |
| PHASE1 | 139 |
| PHASE1/PHASE2 | 82 |
| Not specified | 24 |
| PHASE2/PHASE3 | 20 |
| PHASE4 | 13 |
| EARLY_PHASE1 | 4 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05689671 | PHASE4 | ACTIVE_NOT_RECRUITING | Pemetrexed-free vs. Pemetrexed-based Immunochemotherapy in Metastatic TTF-1 Negative Lung Adenocarcinoma |
| NCT00380718 | PHASE4 | COMPLETED | Chemotherapy for Patients With Non-Small Cell Lung Cancer |
| NCT01020786 | PHASE4 | COMPLETED | A Study in Non-squamous Non Small Cell Lung Cancer in Asian Patients |
| NCT01442909 | PHASE4 | COMPLETED | Pemetrexed Followed by Docetaxel or in Reverse Sequence |
| NCT02031601 | PHASE4 | UNKNOWN | Intercalated Combination of Chemotherapy and Tyrosine Kinase Inhibitors as First-line Treatment for Patients With Non-Small-Cell Lung Cancer |
| NCT02399566 | PHASE4 | UNKNOWN | Clinical Trial of Erlotinib and Pemetrexed for Maintenance Treatment in Lung Adenocarcinoma |
| NCT03460678 | PHASE4 | TERMINATED | Randomized Comparative Study of Erlotinib and Pemetrexed in the Maintenance Treatment of Advanced Lung Cancer Patients. |
| NCT03607149 | PHASE4 | COMPLETED | Pemetrexed in Maintenance in Patients With Impaired Renal Function, 2 Dose Calculation Strategies |
| NCT03655821 | PHASE4 | TERMINATED | Dose Individualization of Pemetrexed - IMPROVE-II |
| NCT03655834 | PHASE4 | COMPLETED | Dose Individualization of Pemetrexed - IMPROVE-III |
| NCT03656549 | PHASE4 | COMPLETED | Dose Individualization of Pemetrexed - IMPROVE-I |
| NCT03768037 | PHASE4 | UNKNOWN | Anlotinib Plus Pemetrexed or Pemetrexed for Previously Untreated Elderly (>=70) or PS=2 Non-squamous NSCLC |
| NCT03792503 | PHASE4 | WITHDRAWN | Pemetrexed Plus Apatinib Maintenance Treatment in Patients With Non-squamous Non-small Cell Lung Cancer Patients Who Have Not Progressed After 4 Cycles of Induction Chemotherapy of Pemetrexed in Combination With Platinum-based Regimen |
| NCT02453282 | PHASE3 | ACTIVE_NOT_RECRUITING | Phase III Open Label First Line Therapy Study of MEDI 4736 (Durvalumab) With or Without Tremelimumab Versus SOC in Non Small-Cell Lung Cancer (NSCLC) |
| NCT02486718 | PHASE3 | ACTIVE_NOT_RECRUITING | Study to Assess Safety and Efficacy of Atezolizumab (MPDL3280A) Compared to Best Supportive Care Following Chemotherapy in Patients With Lung Cancer [IMpower010] |
| NCT02542293 | PHASE3 | ACTIVE_NOT_RECRUITING | Study of Durvalumab With Tremelimumab Versus SoC as 1st Line Therapy in Metastatic Non Small-Cell Lung Cancer (NSCLC) (NEPTUNE) |
| NCT03003962 | PHASE3 | ACTIVE_NOT_RECRUITING | Study of Durvalumab Alone or Chemotherapy for Patients With Advanced Non Small-Cell Lung Cancer (PEARL) |
| NCT03164616 | PHASE3 | ACTIVE_NOT_RECRUITING | Study of Durvalumab + Tremelimumab With Chemotherapy or Durvalumab With Chemotherapy or Chemotherapy Alone for Patients With Lung Cancer (POSEIDON). |
| NCT03178552 | PHASE2/PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Evaluate the Efficacy and Safety of Multiple Targeted Therapies as Treatments for Participants With Non-Small Cell Lung Cancer (NSCLC) |
| NCT03425643 | PHASE3 | ACTIVE_NOT_RECRUITING | Efficacy and Safety of Pembrolizumab (MK-3475) With Platinum Doublet Chemotherapy as Neoadjuvant/Adjuvant Therapy for Participants With Resectable Stage II, IIIA, and Resectable IIIB (T3-4N2) Non-small Cell Lung Cancer (MK-3475-671/KEYNOTE-671) |
| NCT03456076 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study Comparing Adjuvant Alectinib Versus Adjuvant Platinum-Based Chemotherapy in Patients With ALK Positive Non-Small Cell Lung Cancer |
| NCT03519971 | PHASE3 | ACTIVE_NOT_RECRUITING | Study of Durvalumab Given With Chemoradiation Therapy in Patients With Unresectable Non-small Cell Lung Cancer |
| NCT03768063 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study in Patients Previously Enrolled in a Genentech and/or F. Hoffmann-La Roche Ltd Sponsored Atezolizumab Study |
| NCT03793179 | PHASE3 | ACTIVE_NOT_RECRUITING | Testing the Timing of Pembrolizumab Alone or With Chemotherapy as First Line Treatment and Maintenance in Non-small Cell Lung Cancer |
| NCT03800134 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Neoadjuvant/Adjuvant Durvalumab for the Treatment of Patients With Resectable Non-small Cell Lung Cancer |
| NCT04025879 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Neoadjuvant Chemotherapy Plus Nivolumab Versus Neoadjuvant Chemotherapy Plus Placebo, Followed by Surgical Removal and Adjuvant Treatment With Nivolumab or Placebo for Participants With Surgically Removable Early Stage Non-small Cell Lung Cancer |
| NCT04035486 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Osimertinib With or Without Chemotherapy as 1st Line Treatment in Patients With Mutated Epidermal Growth Factor Receptor Non-Small Cell Lung Cancer (FLAURA2) |
| NCT04129502 | PHASE3 | ACTIVE_NOT_RECRUITING | TAK-788 as First-Line Treatment Versus Platinum-Based Chemotherapy for Non-Small Cell Lung Cancer (NSCLC) With EGFR Exon 20 Insertion Mutations |
| NCT04194944 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Selpercatinib (LY3527723) in Participants With Advanced or Metastatic RET Fusion-Positive Non-Small Cell Lung Cancer |
| NCT04205812 | PHASE3 | ACTIVE_NOT_RECRUITING | Platinum-Based Chemotherapy With/Without INCMGA00012, an Anti-PD-1 Antibody, in Non-Small Cell Lung Cancer |
| NCT04339218 | PHASE3 | RECRUITING | Cryoablation in Combination (or Not) With Pembrolizumab and Pemetrexed-carboplatin in 1st-line Treatment for Patients With Metastatic Lung Adenocarcinoma |
| NCT04351555 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Osimertinib With or Without Chemotherapy Versus Chemotherapy Alone as Neoadjuvant Therapy for Patients With EGFRm Positive Resectable Non-Small Cell Lung Cancer |
| NCT04380636 | PHASE3 | ACTIVE_NOT_RECRUITING | Study of Pembrolizumab With Concurrent Chemoradiation Therapy Followed by Pembrolizumab With or Without Olaparib in Stage III Non-Small Cell Lung Cancer (NSCLC) (MK-7339-012/KEYLYNK-012) |
| NCT04538664 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Combination Amivantamab and Carboplatin-Pemetrexed Therapy, Compared With Carboplatin-Pemetrexed, in Participants With Advanced or Metastatic Non-Small Cell Lung Cancer Characterized by Epidermal Growth Factor Receptor (EGFR) Exon 20 Insertions |
| NCT04585490 | PHASE3 | RECRUITING | Personalized Escalation of Consolidation Treatment Following Chemoradiotherapy and Immunotherapy in Stage III NSCLC in Stage III NSCLC |
| NCT04695925 | PHASE3 | ACTIVE_NOT_RECRUITING | Osimertinib Monotherapy or Combination With Chemotherapy for Advanced NSCLC Concurrent EGFR and TP53 Mutations |
| NCT04762459 | PHASE3 | ENROLLING_BY_INVITATION | Efficacy and Safety of Almonertinib Combined With or Without Chemotherapy as an Adjuvant Treatment for Stage II-IIIA Non-small Cell Lung Carcinoma Following Complete Tumour Resection |
| NCT04956692 | PHASE3 | ACTIVE_NOT_RECRUITING | Study of Pembrolizumab (MK-3475) Subcutaneous (SC) Versus Pembrolizumab Intravenous (IV) Administered With Platinum Doublet Chemotherapy in Participants With Metastatic Squamous or Nonsquamous Non-Small Cell Lung Cancer (NSCLC) (MK-3475-A86) |
| NCT04988295 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Amivantamab and Lazertinib in Combination With Platinum-Based Chemotherapy Compared With Platinum-Based Chemotherapy in Patients With Epidermal Growth Factor Receptor (EGFR)-Mutated Locally Advanced or Metastatic Non- Small Cell Lung Cancer After Osimertinib Failure |
| NCT05048797 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Investigate the Efficacy and Safety of Trastuzumab Deruxtecan as the First Treatment Option for Unresectable, Locally Advanced/Metastatic Non-Small Cell Lung Cancer With HER2 Mutations |
Clinical evidence (CIViC)
Variant × indication × effect (13 predictive associations from 14 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| EGFR L858R OR EGFR Exon 19 Deletion | Lung Non-small Cell Carcinoma | Sensitivity/Response | Carboplatin + Pemetrexed + Amivantamab | CIViC A | EID12156 |
| ALK Fusion | Lung Non-small Cell Carcinoma | Sensitivity/Response | Pemetrexed | CIViC B | EID945 |
| EGFR Mutation | Lung Non-small Cell Carcinoma | Sensitivity/Response | Pemetrexed + Gefitinib | CIViC B | EID7650 |
| KRAS Mutation | Lung Non-small Cell Carcinoma | Sensitivity/Response | Pemetrexed + Docetaxel + Trametinib | CIViC B | EID4862 |
| MTAP Deletion | Bladder Urothelial Carcinoma | Sensitivity/Response | Pemetrexed | CIViC B | EID12722 |
| MTAP Underexpression AND CDKN2A Underexpression | Lung Adenocarcinoma | Sensitivity/Response | Pemetrexed | CIViC B | EID12723 |
| TYMS Underexpression | Lung Non-small Cell Carcinoma | Sensitivity/Response | Pemetrexed | CIViC B | EID907 |
| TYMS Overexpression | Lung Non-small Cell Carcinoma | Resistance | Pemetrexed | CIViC B | EID832 +1 |
| MDM2 EXPRESSION | Malignant Pleural Mesothelioma | Resistance | Pemetrexed + Cisplatin | CIViC B | EID827 |
| TYMS Amplification | Lung Adenocarcinoma | Resistance | Pemetrexed | CIViC B | EID903 |
| EGFR T790M | Lung Non-small Cell Carcinoma | Sensitivity/Response | Erlotinib + Pemetrexed | CIViC C | EID277 |
| MET Exon 14 Skipping Mutation AND CD274 Overexpression | Lung Adenocarcinoma | Sensitivity/Response | Carboplatin + Pemetrexed | CIViC C | EID11397 |
| TYMS Underexpression | Prostate Cancer | Sensitivity/Response | Pemetrexed | CIViC C | EID908 |
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
28 molecules share ≥1 primary target. Top 28 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| METHOTREXATE | ChEMBL + PubChem | Phase 4 (approved) | DHFR, GART, TYMS |
| Folic Acid | ChEMBL + PubChem | Phase 4 (approved) | DHFR, TYMS |
| PRALATREXATE | ChEMBL + PubChem | Phase 4 (approved) | DHFR, GART |
| RALTITREXED | ChEMBL | Phase 4 (approved) | DHFR, TYMS |
| LEUCOVORIN | ChEMBL + PubChem | Phase 4 (approved) | DHFR |
| DIFLUNISAL | ChEMBL | Phase 4 (approved) | DHFR |
| GENTAMICIN | ChEMBL | Phase 4 (approved) | DHFR |
| MEFENAMIC ACID | ChEMBL | Phase 4 (approved) | DHFR |
| PHENOLPHTHALEIN | ChEMBL | Phase 4 (approved) | TYMS |
| PYRIMETHAMINE | ChEMBL | Phase 4 (approved) | DHFR |
| SULFACETAMIDE | ChEMBL | Phase 4 (approved) | DHFR |
| SULFADIAZINE | ChEMBL | Phase 4 (approved) | DHFR |
| TERIFLUNOMIDE | ChEMBL | Phase 4 (approved) | DHFR |
| TRIMETHOPRIM | ChEMBL | Phase 4 (approved) | DHFR |
| TRIMETREXATE | ChEMBL | Phase 4 (approved) | DHFR |
| ICLAPRIM | ChEMBL | Phase 3 | DHFR |
| NOLATREXED | ChEMBL | Phase 3 | TYMS |
| AMINOPTERIN | ChEMBL | Phase 2 | DHFR |
| BREQUINAR | ChEMBL | Phase 2 | DHFR |
| CYCLOGUANIL | ChEMBL | Phase 2 | DHFR |
| DIAVERIDINE | ChEMBL | Phase 2 | DHFR |
| EDATREXATE | ChEMBL | Phase 2 | DHFR |
| EPIROPRIM | ChEMBL | Phase 2 | DHFR |
| LOMETREXOL | ChEMBL | Phase 2 | GART |
| METESIND | ChEMBL | Phase 2 | TYMS |
| OSI-7904 | ChEMBL | Phase 2 | TYMS |
| PIRITREXIM | ChEMBL | Phase 2 | DHFR |
| Pemetrexed Disodium | PubChem | Approved | TYMS |
Related Atlas pages
- Genes: DHFR, GART, TYMS
- Diseases: neoplasm, mesothelioma, malignant pleural mesothelioma, malignant peritoneal mesothelioma, non-small cell lung carcinoma, gastric carcinoma, carcinoma, lung adenocarcinoma, small cell lung carcinoma, gastric neoplasm, upper aerodigestive tract neoplasm, head and neck cancer, lung neoplasm, cervical adenocarcinoma, bladder transitional cell carcinoma, prostate carcinoma
- Drugs: Methotrexate, Folic Acid, Pralatrexate, Raltitrexed, Diflunisal, Gentamicin, Mefenamic Acid, Phenolphthalein, Pyrimethamine, Sulfacetamide, Sulfadiazine, Teriflunomide, Trimethoprim, Trimetrexate, Iclaprim, Nolatrexed
- Biomarker genes: MTAP