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Methotrexate

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Also known as (r)-methotrexateADX-2191AmethopterinCL 14377CL-14377D-amethopterinD-methotrexateEbetrexEMT-25299Emtexate high-potEmtexate pfJylamvoMaxtrexMethotrexate, (r)-d-MethotrexatumMethylaminopterinMetojectMetotrexato

Summary

Methotrexate (CHEMBL34259) is an approved small-molecule antineoplastic agent (ATC L04AX03) targeting SLC19A1 and SLC46A1; indicated across 164 conditions including rheumatoid arthritis and psoriasis; with CIViC clinical evidence for 14 variant-indication associations (e.g. IKZF1 Deletion in b-lymphoblastic leukemia/lymphoma).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L04AX03 (+1 more)
  • Targets: 2 (SLC19A1, SLC46A1)
  • Indications: 164 conditions
  • Clinical trials: 1,300
  • Precision-oncology evidence (CIViC): 14 variant–indication associations
  • Chemistry: 454.4 Da · C20H22N8O5

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL34259
NameMethotrexate
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID126941
ChEBICHEBI:44185
ATCL04AX03, L01BA01
Molecular formulaC20H22N8O5
Molecular weight454.4
InChIKeyFBOZXECLQNJBKD-ZDUSSCGKSA-N

SMILES: CN(CC1=CN=C2C(=N1)C(=NC(=N2)N)N)C3=CC=C(C=C3)C(=O)N[C@@H](CCC(=O)O)C(=O)O

IUPAC name: (2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methylamino]benzoyl]amino]pentanedioic acid

Pharmacological roles (ChEBI): antineoplastic agent, antirheumatic drug, EC 1.5.1.3 (dihydrofolate reductase) inhibitor, DNA synthesis inhibitor, abortifacient, dermatologic drug, immunosuppressive agent.

Other ChEBI roles (chemical / environmental): antimetabolite.

Also known as: (r)-methotrexate, ADX-2191, Amethopterin, CL 14377, CL-14377, D-amethopterin, D-methotrexate, Ebetrex, EMT-25299, Emtexate high-pot, Emtexate pf, Jylamvo

Parent form; salt/anhydrous children: CHEMBL1376974, CHEMBL3244648

Patent coverage: 102,924 distinct patent families (398,396 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 392,229 (98%) 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).

GeneTargetActionpAffinityCancer dependencyUniProt
SLC19A1Reduced folate transporter 131.4%P41440
SLC46A1Proton-coupled folate transporter2.7%Q96NT5

Broader ChEMBL bioactivity targets: 51 (assay-derived). Sample: Dihydrofolate reductase, Tyrosyl-DNA phosphodiesterase 1, Bifunctional dihydrofolate reductase-thymidylate synthase, Microtubule-associated protein tau, Lysine-specific demethylase 4E, Survival motor neuron protein, Prelamin-A/C, RecQ-like DNA helicase BLM, 4’-phosphopantetheinyl transferase ffp, Ferritin light chain.

Bioactivity

ChEMBL activities: 260 potent at pChembl ≥ 5 of 303 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
DHFR11Ki0.01nMCHEMBL_ACT_18251252
P0ABQ410.68Ki0.02nMCHEMBL_ACT_380863
P0ABQ410.64Kd0.02nMCHEMBL_ACT_821579
DHFR10.42Ki0.04nMCHEMBL_ACT_939068
Q920D210.14Ki0.07nMCHEMBL_ACT_3055900
DHFR10.11Ki0.08nMCHEMBL_ACT_3055901
P0ABQ410.02Kd0.1nMCHEMBL_ACT_821582
DHFR9.96Ki0.11nMCHEMBL_ACT_228406
P073829.89Ki0.13nMCHEMBL_ACT_197375
DHFR9.75Ki0.18nMCHEMBL_ACT_939069
DHFR9.22IC500.6nMCHEMBL_ACT_507772
DHFR9.15IC500.7nMCHEMBL_ACT_1263049
DHFR9.14IC500.72nMCHEMBL_ACT_507771
DHFR9.09IC500.82nMCHEMBL_ACT_81456
P139229.05IC500.89nMCHEMBL_ACT_28871366
P161849IC501nMCHEMBL_ACT_1113070
P161849IC501nMCHEMBL_ACT_1165943
P161849IC501nMCHEMBL_ACT_1191604
P0A0179Ki1nMCHEMBL_ACT_16653546
DHFR9IC501nMCHEMBL_ACT_2069335
P161849IC501nMCHEMBL_ACT_818026
Q277938.96IC501.1nMCHEMBL_ACT_28871168
P161848.96IC501.1nMCHEMBL_ACT_412077
DHFR8.93IC501.18nMCHEMBL_ACT_505257
DHFR8.92IC501.2nMCHEMBL_ACT_94090
P161848.89IC501.3nMCHEMBL_ACT_1092730
P161848.89IC501.3nMCHEMBL_ACT_1132177
P161848.89IC501.3nMCHEMBL_ACT_13297327
P003818.89IC501.3nMCHEMBL_ACT_285163
P161848.89IC501.3nMCHEMBL_ACT_73582

Target pathways

Aggregated over 2 target gene(s): SLC19A1, SLC46A1.

Top Reactome pathways

6 total, by targets touching each:

PathwayTargetsGenes
Metabolism of folate and pterines2SLC19A1, SLC46A1
Metabolism1SLC19A1
Metabolism of water-soluble vitamins and cofactors1SLC19A1
Metabolism of vitamins and cofactors1SLC19A1
Iron uptake and transport1SLC46A1
Heme signaling1SLC46A1

Dominant GO biological processes

GO termTargets
folic acid transport2
folic acid metabolic process2
methotrexate transport2
folate transmembrane transport2
folate import across plasma membrane2
xenobiotic transmembrane transport1
female pregnancy1
response to xenobiotic stimulus1
response to toxic substance1
obsolete organic anion transport1
cyclic-GMP-AMP transmembrane import across plasma membrane1
positive regulation of cGAS/STING signaling pathway1
transport across blood-brain barrier1
vitamin transmembrane transport1
vitamin transport1

Indications & clinical

Indications

164 indications (20 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).

IndicationTrial phaseMONDOEFO
rheumatoid arthritis4MONDO:0008383EFO:0000685
psoriasis4MONDO:0005083EFO:0000676
psoriatic arthritis4MONDO:0011849EFO:0003778
acute lymphoblastic leukemia4MONDO:0004967EFO:0000220
juvenile idiopathic arthritis4MONDO:0011429EFO:0002609
immune system disorder4MONDO:0005046EFO:0000540
neoplasm4MONDO:0005070EFO:0000616
mycosis fungoides4MONDO:0009691EFO:1001051
B-cell acute lymphoblastic leukemia4MONDO:0004947EFO:0000094
breast carcinoma4MONDO:0004989EFO:0000305
breast neoplasm4MONDO:0021100EFO:0003869
non-Hodgkin lymphoma4MONDO:0018908EFO:0005952
arthritic joint disease4MONDO:0005578MONDO:0024280
Crohn disease3MONDO:0005011EFO:0000384
head and neck squamous cell carcinoma3MONDO:0010150EFO:0000181
cardiovascular disorder3MONDO:0004995EFO:0000319
hydatidiform mole3MONDO:0006248EFO:1000298
upper aerodigestive tract neoplasm3MONDO:0005398EFO:0004284
atopic eczema3MONDO:0004980EFO:0000274
osteosarcoma3MONDO:0009807EFO:0000637
lymphoma3MONDO:0005062EFO:0000574
acute myeloid leukemia3MONDO:0018874EFO:0000222
alopecia areata3MONDO:0005340EFO:0004192
diffuse large B-cell lymphoma3MONDO:0018905EFO:0000403
uveitis3MONDO:0020283EFO:1001231
neoplasm of mature B-cells3MONDO:0004949EFO:0000096
Hodgkins lymphoma3MONDO:0004952EFO:0000183
myelodysplastic syndrome3MONDO:0018881EFO:0000198
T-cell acute lymphoblastic leukemia3MONDO:0004963EFO:0000209
acute promyelocytic leukemia3MONDO:0012883EFO:0000224
chronic myeloid leukemia3MONDO:0011996EFO:0000339
dermatomyositis3MONDO:0016367EFO:0000398
juvenile dermatomyositis3MONDO:0008054EFO:0000557
leukemia3MONDO:0005059EFO:0000565
sarcoma3MONDO:0005089EFO:0000691
squamous cell carcinoma3MONDO:0005096EFO:0000707
medulloblastoma3MONDO:0007959EFO:0002939
anaplastic large cell lymphoma3MONDO:0020325EFO:0003032
brain neoplasm3MONDO:0021211EFO:0003833
ankylosing spondylitis3MONDO:0005306EFO:0003898
lymphoid leukemia3MONDO:0005402EFO:0004289
graft versus host disease3MONDO:0013730EFO:0004599
primitive neuroectodermal tumor3MONDO:0005462EFO:0005235
granulomatosis with polyangiitis3MONDO:0012105EFO:0005297
head and neck cancer3MONDO:0005627EFO:0006859
bullous pemphigoid3MONDO:0019082EFO:0007187
sensorineural hearing loss disorder3MONDO:0020678EFO:1001176
temporal arteritis3MONDO:0008538EFO:1001209
primary biliary cholangitis3MONDO:0005388EFO:1001486
chronic myelomonocytic leukemia3MONDO:0020311EFO:1001779
precursor T-cell acute lymphoblastic leukemia3MONDO:0020512EFO:1001830
aplastic anemia3MONDO:0015909HP:0001915
vasculitis3MONDO:0018882EFO:0006803
ectopic pregnancy3MONDO:0000755HP:0031456
acute erythroid leukemia3MONDO:0017858EFO:0000218
acute monocytic leukemia3MONDO:0007896EFO:0000221
acute myelomonocytic leukemia M43MONDO:0018871EFO:0000223
myeloproliferative neoplasm3MONDO:0020076EFO:0002428
choriocarcinoma3MONDO:0005207EFO:0002893
acute megakaryoblastic leukemia3MONDO:0018872EFO:0003025
acute myeloblastic leukemia without maturation3MONDO:0005224EFO:0003027
myelodysplastic syndrome with single lineage dysplasia3MONDO:0005272EFO:0003802
myelodysplastic syndrome with excess blasts3MONDO:0019454EFO:0003811
vitiligo3MONDO:0008661EFO:0004208
central nervous system neoplasm3MONDO:0006130EFO:1000158
intermediate uveitis3MONDO:0006806EFO:1000986
brain cancer3MONDO:0001657MONDO:0001657
follicular lymphoma3MONDO:0018906MONDO:0018906
acute biphenotypic leukemia3MONDO:0020322MONDO:0019460
nasal cavity and paranasal sinus lethal midline granuloma3MONDO:0006828MONDO:0019472
urothelial carcinoma3MONDO:0040679EFO:0008528
proliferative vitreoretinopathy3MONDO:0700115EFO:1001129
IgG4-related retroperitoneal fibrosis3MONDO:0018848MONDO:0018848
asthma3MONDO:0004979MONDO:0004979
osteoarthritis3MONDO:0005178MONDO:0005178
multiple sclerosis3MONDO:0005301MONDO:0005301
systemic lupus erythematosus3MONDO:0007915MONDO:0007915
primary cutaneous T-cell non-Hodgkin lymphoma3MONDO:0000607EFO:0002913
ulcerative colitis2MONDO:0005101EFO:0000729
myasthenia gravis2MONDO:0009688EFO:0004991
myocardial infarction2MONDO:0005068EFO:0000612
urticaria2MONDO:0005492EFO:0005531
B-cell chronic lymphocytic leukemia2MONDO:0004948EFO:0000095
peripheral T-cell lymphoma, not otherwise specified2MONDO:0004964EFO:0000211
Burkitt lymphoma2MONDO:0007243EFO:0000309
mesothelioma2MONDO:0005065EFO:0000588
malignant pleural mesothelioma2MONDO:0005112EFO:0000770
ovarian carcinoma2MONDO:0005140EFO:0001075
plasma cell myeloma2MONDO:0009693EFO:0001378
lymphoid neoplasm2MONDO:0005157EFO:0001642
primary myelofibrosis2MONDO:0009692EFO:0002430
juvenile myelomonocytic leukemia2MONDO:0011908EFO:1000309
Langerhans cell histiocytosis2MONDO:0018310EFO:1000318
mantle cell lymphoma2MONDO:0018876EFO:1001469
cutaneous neuroendocrine carcinoma2MONDO:0019210EFO:1001471
angioimmunoblastic T-cell lymphoma2MONDO:0004977EFO:0000255
acquired polycythemia vera2MONDO:0009891EFO:0002429
Waldenstrom macroglobulinemia2MONDO:0100280EFO:0009441
Sezary syndrome2MONDO:0017844EFO:1000785
neuroblastoma2MONDO:0005072EFO:0000621
central serous chorioretinopathy2MONDO:0018616EFO:0009784
blast phase chronic myelogenous leukemia, BCR-ABL1 positive2MONDO:0006115EFO:1000131
kidney cancer2MONDO:0002367MONDO:0002367
ependymoma2MONDO:0016698MONDO:0003478
ovarian cancer2MONDO:0008170MONDO:0008170
hematopoietic and lymphoid system neoplasm2MONDO:0002334MONDO:0044881
coronary artery disorder2MONDO:0005010EFO:0001645
desmoid tumor2MONDO:0007608EFO:0009907
myelodysplastic/myeloproliferative disease2MONDO:0020077MONDO:0020077
MALT lymphoma2MONDO:0007650EFO:0000191
Wiskott-Aldrich syndrome2MONDO:0010518MONDO:0010518
sickle cell disease2MONDO:0011382MONDO:0011382
Diamond-Blackfan anemia2MONDO:0015253MONDO:0015253
severe combined immunodeficiency2MONDO:0015974MONDO:0015974
osteopetrosis2MONDO:0017198MONDO:0017198
neurofibromatosis type 12MONDO:0018975MONDO:0018975
retinitis pigmentosa2MONDO:0019200MONDO:0019200
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
hemoglobinuria2MONDO:0003656MONDO:0100244
plasma cell neoplasm2MONDO:0004959EFO:0000200
testicular cancer2MONDO:0005447EFO:0004281
CD4+/CD56+ hematodermic neoplasm2MONDO:0019467EFO:0010580
colorectal neoplasm2MONDO:0005335MONDO:0005575
malaria1MONDO:0005136EFO:0001068
systemic sclerosis1MONDO:0005100EFO:0000717
cutaneous melanoma1MONDO:0005012EFO:0000389
HIV infectious disease1MONDO:0005109EFO:0000764
plasma cell leukemia1MONDO:0018689EFO:0006475
severe acute respiratory syndrome1MONDO:0005091MONDO:0100096
Fanconi anemia1MONDO:0019391MONDO:0019391
gout1MONDO:0005393EFO:0004274
dermatitis0MONDO:0002406MONDO:0002406

32 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 1,300.

Phase distribution

PhaseTrials
PHASE2484
PHASE3312
PHASE4169
Not specified124
PHASE195
PHASE1/PHASE268
PHASE2/PHASE333
EARLY_PHASE115

Top trials by phase / activity

NCTPhaseStatusTitle
NCT02714634PHASE4RECRUITINGClinical Trial Evaluating Methotrexate or Leflunomide + Targeted Therapy Versus Methotrexate or Leflunomide + Sulfasalazine + Hydroxychloroquine in Patients With Rheumatoid Arthritis and Insufficient Response to Methotrexate or Leflunomide
NCT04239859PHASE4NOT_YET_RECRUITINGOutcomes With Treatment and Withdraw of Secukinumab in Patients With Plaque Psoriasis
NCT04314193PHASE4ACTIVE_NOT_RECRUITINGEffectiveness of Methotrexate Versus Prednisone as First-line Therapy for Pulmonary Sarcoidosis
NCT04537689PHASE4RECRUITINGOutcomes With Treatment and Withdraw of Ixekizumab in Patients With Plaque Psoriasis
NCT04579848PHASE4ACTIVE_NOT_RECRUITINGMethotrexate in Erosive Inflammatory Hand Osteoarthritis
NCT05102448PHASE4RECRUITINGComparison of Tofacitinib and Methotrexate in Takayasu’s Arteritis
NCT05353829PHASE4ACTIVE_NOT_RECRUITINGMethotrexate in Patients with Early Rheumatoid Arthritis
NCT05518383PHASE4RECRUITINGB-cell Mature Non-Hodgkin’s Lymphoma Treatment Protocol in Children and Adolescents 2021
NCT05626348PHASE4RECRUITINGThe Clinical Efficacy of Immunomodulators in RA Patients
NCT06289673PHASE4RECRUITINGIdentification of Necessary Information for Treatment Induction in Newly Diagnosed Acute Lymphoblastic Leukemia/Lymphoma
NCT06498089PHASE4RECRUITINGA Randomized, Controlled, Open-label, Multicenter Clinical Trial Comparing the Efficacy and Safety of a Precision Treatment Regimen Based on Clinical-molecular Phenotypes with a Conventional Treatment Regimen in the Treatment of Patients with Active Takayasu’s Arteritis
NCT06578728PHASE4ACTIVE_NOT_RECRUITINGLocal Methotrexate Injections for the Treatment of Nail Psoriasis
NCT06649136PHASE4RECRUITINGMethMax Trial: MAXimising the METHotrexate Therapy Potential in Patients with Active Rheumatoid Arthritis
NCT06653634PHASE4RECRUITINGOptimizing Treatment for Patients With Juvenile Idiopathic Arthritis in Sustained Remission: The MOVE-JIA Trial
NCT06913907PHASE4RECRUITINGChanges in MTX-PG Concentrations During Subcutaneous MTX Therapy in Patients With Rheumatoid Arthritis(COSMOS Study)
NCT06943482PHASE4NOT_YET_RECRUITINGComparing Effectiveness of Steroids and Methotrexate in Treatment of Chronic Inflammatory Breast Disease
NCT07352566PHASE4NOT_YET_RECRUITINGUtilization of a Microdevice for Psoriasis and Atopic Dermatitis
NCT07381556PHASE4RECRUITINGCyclosporine Or Methotrexate for Pediatric Alopecia Areata: Routine Clinical Care Effectiveness Study
NCT07406204PHASE4NOT_YET_RECRUITINGTofacitinib vs Methotrexate for Severe Alopecia Areata (TOFA-MTX-AA)
NCT07432386PHASE4NOT_YET_RECRUITINGMethotrexate Versus Apremilast for Pruritus in Psoriasis
NCT07432815PHASE4RECRUITINGTreatment of Psoriasis With Depression and/or Anxiety With Methotrexate vs Combined Methotrexate and Antidepressant
NCT07459933PHASE4NOT_YET_RECRUITINGTopical Methotrexate vs Minoxidil for Localized Alopecia Areata
NCT07477691PHASE4NOT_YET_RECRUITINGImmune Modulation During Palynziq® Treatment in Adults (IMPALA)
NCT00029523PHASE4COMPLETEDDepoCyt Therapy in Patients With Neoplastic Meningitis From Lymphoma or a Solid Tumor
NCT00037102PHASE4COMPLETEDCombination Therapy With Avonex and BiMonthly High Dose Intravenous Methotrexate in Multiple Sclerosis
NCT00037115PHASE4WITHDRAWNInduction Therapy With a Single High Dose Bolus of Intravenous Methotrexate With Leucovorin Rescue, Prior to Initiation of AVONEX® Treatment, in Patients Presenting With a First Acute Demyelinating Event.
NCT00112034PHASE4COMPLETEDAVONEX® Combination Trial - ACT
NCT00129506PHASE4COMPLETEDComparing Methotrexate Followed by Misoprostol to Misoprostol Alone for Early Abortion
NCT00153530PHASE4COMPLETEDWhole Brain Irradiation in Primary Central Nervous System (CNS) Lymphoma (PCNSL)
NCT00161655PHASE4COMPLETEDStudy Evaluating Etanercept and Methotrexate in Plaque Psoriasis
NCT00195494PHASE4COMPLETEDStudy Comparing Etanercept and Methotrexate vs. Methotrexate Alone in Rheumatoid Arthritis
NCT00198978PHASE4COMPLETEDGerman Multicenter Trial for Treatment of Elderly Patients With Newly Diagnosed Acute Lymphoblastic Leukemia
NCT00198991PHASE4COMPLETEDGerman Multicenter Trial for Treatment of Newly Diagnosed Acute Lymphoblastic Leukemia in Adults (07/2003)
NCT00199004PHASE4COMPLETEDTrial for Treatment of Adult Patients With Standard Risk Acute Lymphoblastic Leukemia With Chemotherapy and Rituximab
NCT00199017PHASE4COMPLETEDGerman Multicenter Trial for the Treatment of Newly Diagnosed T-lymphoblastic Lymphoma in Adults
NCT00199056PHASE4COMPLETEDGerman Multicenter Trial for Treatment of Newly Diagnosed Acute Lymphoblastic Leukemia in Adults (06/99)
NCT00199069PHASE4COMPLETEDGerman Multicenter Trial for Treatment of Newly Diagnosed Acute Lymphoblastic Leukemia in Adults (05/93)
NCT00199082PHASE4COMPLETEDNewly Diagnosed Mature B-ALL, Burkitt’s Lymphoma and Other High-grade Lymphoma in Adults
NCT00199095PHASE4COMPLETEDTreatment of Elderly Patients (>65 Years) With Acute Lymphoblastic Leukemia
NCT00209859PHASE4COMPLETEDMethotrexate and Cyclosporine in Treatment of Early Rheumatoid Arthritis

Clinical evidence (CIViC)

Variant × indication × effect (14 predictive associations from 14 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
IKZF1 DeletionB-lymphoblastic Leukemia/lymphomaSensitivity/ResponseMethotrexate + Daunorubicin + Cytarabine + Fludarabine + ImatinibCIViC BEID7366
SLCO1B1 N130DCancerAdverse ResponseMethotrexateCIViC BEID1842
SLCO1B1 RS4149056CancerAdverse ResponseMethotrexateCIViC BEID1841
TYMS RS34743033CancerAdverse ResponseMethotrexateCIViC BEID1843
ETV6::NTRK3 FusionB-lymphoblastic Leukemia/lymphomaSensitivity/ResponseEtoposide + Methotrexate + LarotrectinibCIViC CEID8917
PRPS1 A190TB-lymphoblastic Leukemia/lymphomaResistanceCytarabine + Asparaginase + Methotrexate + DaunorubicinCIViC DEID7928
PRPS1 D183EB-lymphoblastic Leukemia/lymphomaResistanceAsparaginase + Methotrexate + Cytarabine + DaunorubicinCIViC DEID7927
PRPS1 K176NB-lymphoblastic Leukemia/lymphomaResistanceDaunorubicin + Cytarabine + Methotrexate + AsparaginaseCIViC DEID7926
PRPS1 L191FB-lymphoblastic Leukemia/lymphomaResistanceAsparaginase + Daunorubicin + MethotrexateCIViC DEID7923
PRPS1 N144SB-lymphoblastic Leukemia/lymphomaResistanceDaunorubicin + Methotrexate + AsparaginaseCIViC DEID7930
PRPS1 S103NB-lymphoblastic Leukemia/lymphomaResistanceMethotrexate + Asparaginase + Daunorubicin + CytarabineCIViC DEID7925
PRPS1 S103TB-lymphoblastic Leukemia/lymphomaResistanceMethotrexate + Asparaginase + Daunorubicin + CytarabineCIViC DEID7924
PRPS1 T303SB-lymphoblastic Leukemia/lymphomaResistanceAsparaginase + Daunorubicin + Cytarabine + MethotrexateCIViC DEID7929
TP53 R273HOsteosarcomaResistanceDoxorubicin + MethotrexateCIViC DEID7430

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (2) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

GuidelineSourceGene(s)DosingRecommendation
Annotation of RNPGx Guideline for methotrexate and ABCB1, MTHFR, SLC19RNPGxABCB1;MTHFR;SLC19A1;SLCO1B1
Annotation of DPWG Guideline for methotrexate and MTHFRDPWGMTHFR

PharmGKB also curates 175 clinical and 1,054 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

5 molecules share ≥1 primary target. Top 5 by shared-target count:

MoleculeSourceStatusShared targets
PEMETREXEDChEMBL + PubChemPhase 4 (approved)SLC19A1, SLC46A1
PRALATREXATEChEMBL + PubChemPhase 4 (approved)SLC19A1, SLC46A1
RALTITREXEDChEMBLPhase 4 (approved)SLC19A1, SLC46A1
IndomethacinPubChemApprovedSLC46A1
LeucovorinPubChemApprovedSLC19A1

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot