Pyrimethamine
drug drugOn this page
Also known as ChloridineDaraprimGNF-PF-5586MalacideNSC-3061PirimetaminaPyrimethamine component of fansidarPyrimethaminumRP-4753TCMDC-123831TCMDC-125860WR-2978PYRSID11112140SID17389746SID26747011SID855854SID56422411SID104171273
Summary
Pyrimethamine (CHEMBL36) is an approved small-molecule EC 1.5.1.3 (dihydrofolate reductase) inhibitor (ATC P01BD01) targeting SLC47A1 and SLC47A2; indicated across 23 conditions including malaria and toxoplasmosis.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: P01BD01 (+1 more)
- Targets: 2 (SLC47A1, SLC47A2)
- Indications: 23 conditions
- Clinical trials: 51
- Chemistry: 248.71 Da · C12H13ClN4
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL36 |
| Name | Pyrimethamine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 4993 |
| ChEBI | CHEBI:8673 |
| ATC | P01BD01, P01BD51 |
| Molecular formula | C12H13ClN4 |
| Molecular weight | 248.71 |
| InChIKey | WKSAUQYGYAYLPV-UHFFFAOYSA-N |
SMILES: CCC1=C(C(=NC(=N1)N)N)C2=CC=C(C=C2)Cl
IUPAC name: 5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
ChEBI definition: An aminopyrimidine that is pyrimidine-2,4-diamine which is substituted at position 5 by a p-chlorophenyl group and at position 6 by an ethyl group. It is a folic acid antagonist used as an antimalarial or with a sulfonamide to treat toxoplasmosis.
Pharmacological roles (ChEBI): antimalarial, EC 1.5.1.3 (dihydrofolate reductase) inhibitor, antiprotozoal drug.
Also known as: Chloridine, Daraprim, GNF-PF-5586, Malacide, NSC-3061, Pirimetamina, Pyrimethamine, Pyrimethamine component of fansidar, Pyrimethaminum, RP-4753, TCMDC-123831, TCMDC-125860
Patent coverage: 6,205 distinct patent families (19,344 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 19,292 (100%) 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 |
|---|---|---|---|---|---|
| SLC47A1 | Multidrug and toxin extrusion | Inhibition | 7.1 | 0.5% | Q96FL8 |
| SLC47A2 | MATE2 | Inhibition | 6.3 | 0.6% | Q86VL8 |
| Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase | 5.17 |
Broader ChEMBL bioactivity targets: 36 (assay-derived). Sample: Dihydrofolate reductase, Tyrosyl-DNA phosphodiesterase 1, Bifunctional dihydrofolate reductase-thymidylate synthase, Beta-hexosaminidase subunit alpha, Streptokinase A, Survival motor neuron protein, Prelamin-A/C, Dihydrofolate reductase, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Dihydrofolate reductase, Bifunctional dihydrofolate reductase-thymidylate synthase, Dihydrofolate reductase, Solute carrier family 22 member 1, Menin/Histone-lysine N-methyltransferase MLL, 5-hydroxytryptamine receptor 1A, 5-hydroxytryptamine receptor 2A, Alpha-1A adrenergic receptor, Dihydrofolate reductase, Dihydrofolate reductase.
Bioactivity
ChEMBL activities: 115 potent at pChembl ≥ 5 of 137 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| P13922 | 9.72 | Ki | 0.19 | nM | CHEMBL_ACT_1203299 |
| P13922 | 9.22 | Ki | 0.6 | nM | CHEMBL_ACT_1135242 |
| P13922 | 9.22 | Ki | 0.6 | nM | CHEMBL_ACT_955201 |
| P13922 | 9.06 | Ki | 0.87 | nM | CHEMBL_ACT_1464730 |
| P0ABQ4 | 8.92 | Ki | 1.2 | nM | CHEMBL_ACT_1203298 |
| P0ABQ4 | 8.85 | Kd | 1.4 | nM | CHEMBL_ACT_1203292 |
| P13922 | 8.85 | Ki | 1.4 | nM | CHEMBL_ACT_797696 |
| P0ABQ4 | 8.82 | Kd | 1.5 | nM | CHEMBL_ACT_1203290 |
| P13922 | 8.82 | Ki | 1.5 | nM | CHEMBL_ACT_220986 |
| P13922 | 8.82 | Ki | 1.5 | nM | CHEMBL_ACT_797694 |
| P13922 | 8.7 | Ki | 2 | nM | CHEMBL_ACT_1203300 |
| P13922 | 8.44 | Ki | 3.6 | nM | CHEMBL_ACT_797697 |
| P0ABQ4 | 8.28 | Ki | 5.2 | nM | CHEMBL_ACT_1203296 |
| P13922 | 8.28 | IC50 | 5.25 | nM | CHEMBL_ACT_28871372 |
| P13922 | 8.22 | Ki | 6 | nM | CHEMBL_ACT_797695 |
| DHFR | 8.1 | Ki | 8 | nM | CHEMBL_ACT_955214 |
| P16184 | 8.01 | Ki | 9.7 | nM | CHEMBL_ACT_80276 |
| P0ABQ4 | 8 | Ki | 10 | nM | CHEMBL_ACT_1203295 |
| DHFR | 7.96 | Ki | 11 | nM | CHEMBL_ACT_225849 |
| P0ABQ4 | 7.89 | Kd | 13 | nM | CHEMBL_ACT_1203289 |
| P0ABQ4 | 7.8 | Kd | 16 | nM | CHEMBL_ACT_1203291 |
| P0ABQ4 | 7.7 | Ki | 20 | nM | CHEMBL_ACT_1203297 |
| P13922 | 7.59 | IC50 | 25.5 | nM | CHEMBL_ACT_18465860 |
| DHFR | 7.55 | Ki | 28.2 | nM | CHEMBL_ACT_18946332 |
| DHFR | 7.55 | Ki | 28.3 | nM | CHEMBL_ACT_19288990 |
| P13922 | 7.54 | Ki | 28.6 | nM | CHEMBL_ACT_955203 |
| DHFR | 7.51 | Ki | 30.8 | nM | CHEMBL_ACT_3514330 |
| P13922 | 7.27 | Ki | 53.9 | nM | CHEMBL_ACT_955206 |
| P13922 | 7.24 | IC50 | 58 | nM | CHEMBL_ACT_18465802 |
| P13922 | 7.17 | Ki | 67.1 | nM | CHEMBL_ACT_1135243 |
| P13922 | 7.14 | Ki | 71.7 | nM | CHEMBL_ACT_220987 |
| P13922 | 7.1 | IC50 | 80 | nM | CHEMBL_ACT_1135249 |
| P13922 | 7.1 | IC50 | 80 | nM | CHEMBL_ACT_1751611 |
| Q07422 | 7.1 | IC50 | 80 | nM | CHEMBL_ACT_2559293 |
| DHFR | 7.01 | Ki | 98 | nM | CHEMBL_ACT_225848 |
| P00376 | 7 | IC50 | 100.7 | nM | CHEMBL_ACT_18210700 |
| P00376 | 7 | IC50 | 100.7 | nM | CHEMBL_ACT_18259256 |
| P13922 | 6.95 | Ki | 112 | nM | CHEMBL_ACT_1135245 |
| DHFR | 6.92 | Ki | 120 | nM | CHEMBL_ACT_225850 |
| Q07422 | 6.86 | IC50 | 139 | nM | CHEMBL_ACT_19365591 |
| P00376 | 6.85 | IC50 | 141 | nM | CHEMBL_ACT_25601702 |
| Q8K0H1 | 6.84 | Ki | 145 | nM | CHEMBL_ACT_13853423 |
| Q07422 | 6.7 | IC50 | 200 | nM | CHEMBL_ACT_10944969 |
| Q07422 | 6.64 | IC50 | 230 | nM | CHEMBL_ACT_16793600 |
| DHFR | 6.6 | Ki | 250 | nM | CHEMBL_ACT_225847 |
| P0ABQ4 | 6.55 | Ki | 281.8 | nM | CHEMBL_ACT_1168173 |
| P13922 | 6.42 | Ki | 385 | nM | CHEMBL_ACT_1135247 |
| P13922 | 6.42 | Ki | 380 | nM | CHEMBL_ACT_797698 |
| Q07422 | 6.41 | IC50 | 390 | nM | CHEMBL_ACT_1040396 |
| Q07422 | 6.41 | IC50 | 390 | nM | CHEMBL_ACT_1261656 |
| Q07422 | 6.41 | IC50 | 390 | nM | CHEMBL_ACT_177406 |
| Q07422 | 6.41 | IC50 | 390 | nM | CHEMBL_ACT_228327 |
| Q07422 | 6.41 | IC50 | 390 | nM | CHEMBL_ACT_256272 |
| Q07422 | 6.41 | IC50 | 390 | nM | CHEMBL_ACT_560129 |
| Q07422 | 6.41 | IC50 | 390 | nM | CHEMBL_ACT_661044 |
| Q07422 | 6.41 | IC50 | 390 | nM | CHEMBL_ACT_990668 |
| DHFR | 6.4 | IC50 | 400 | nM | CHEMBL_ACT_13297380 |
| DHFR | 6.33 | Ki | 470 | nM | CHEMBL_ACT_18251963 |
| KCNH2 | 6.19 | AC50 | 649 | nM | CHEMBL_ACT_25118001 |
| DHFR | 6.12 | IC50 | 760 | nM | CHEMBL_ACT_19365657 |
| P13922 | 6.07 | Ki | 860 | nM | CHEMBL_ACT_797699 |
| Q27793 | 6 | IC50 | 1000 | nM | CHEMBL_ACT_28871174 |
| Q920D2 | 5.85 | IC50 | 1400 | nM | CHEMBL_ACT_600941 |
| Q920D2 | 5.82 | IC50 | 1500 | nM | CHEMBL_ACT_13297296 |
| Q920D2 | 5.82 | IC50 | 1500 | nM | CHEMBL_ACT_177404 |
| DHFR | 5.78 | IC50 | 1680 | nM | CHEMBL_ACT_19365560 |
| SMN1 | 5.75 | Potency | 1778 | nM | CHEMBL_ACT_3890837 |
| P0ABQ4 | 5.7 | IC50 | 2000 | nM | CHEMBL_ACT_2559273 |
| SLC6A3 | 5.66 | AC50 | 2200 | nM | CHEMBL_ACT_25124042 |
| Q920D2 | 5.64 | IC50 | 2300 | nM | CHEMBL_ACT_1040395 |
| Q920D2 | 5.64 | IC50 | 2300 | nM | CHEMBL_ACT_1261654 |
| Q920D2 | 5.64 | IC50 | 2300 | nM | CHEMBL_ACT_228326 |
| Q920D2 | 5.64 | IC50 | 2300 | nM | CHEMBL_ACT_256270 |
| Q920D2 | 5.64 | IC50 | 2300 | nM | CHEMBL_ACT_661043 |
| Q920D2 | 5.64 | IC50 | 2300 | nM | CHEMBL_ACT_80277 |
| Q920D2 | 5.64 | IC50 | 2300 | nM | CHEMBL_ACT_990666 |
| P16184 | 5.62 | IC50 | 2400 | nM | CHEMBL_ACT_13297324 |
| P16184 | 5.62 | IC50 | 2400 | nM | CHEMBL_ACT_177405 |
| DHFR | 5.58 | IC50 | 2600 | nM | CHEMBL_ACT_515175 |
| P16184 | 5.55 | IC50 | 2800 | nM | CHEMBL_ACT_80275 |
| HEXA | 5.51 | IC50 | 3100 | nM | CHEMBL_ACT_15606671 |
| P16184 | 5.44 | IC50 | 3650 | nM | CHEMBL_ACT_1040394 |
| O08966 | 5.44 | Ki | 3600 | nM | CHEMBL_ACT_13853422 |
| P16184 | 5.44 | IC50 | 3650 | nM | CHEMBL_ACT_228325 |
| P16184 | 5.43 | IC50 | 3700 | nM | CHEMBL_ACT_1261655 |
| P16184 | 5.43 | IC50 | 3700 | nM | CHEMBL_ACT_256271 |
| P16184 | 5.43 | IC50 | 3700 | nM | CHEMBL_ACT_990667 |
| ADRA1A | 5.4 | AC50 | 4000 | nM | CHEMBL_ACT_25137991 |
| P10520 | 5.4 | EC50 | 3992 | nM | CHEMBL_ACT_4885730 |
| DHFR | 5.39 | IC50 | 4074 | nM | CHEMBL_ACT_28871171 |
| DHFR | 5.39 | IC50 | 4074 | nM | CHEMBL_ACT_28871237 |
| DHFR | 5.39 | IC50 | 4074 | nM | CHEMBL_ACT_28871303 |
| DHFR | 5.39 | IC50 | 4074 | nM | CHEMBL_ACT_28871369 |
| DHFR | 5.38 | IC50 | 4169 | nM | CHEMBL_ACT_28870871 |
| DHFR | 5.37 | IC50 | 4300 | nM | CHEMBL_ACT_16793576 |
| HEXB | 5.35 | IC50 | 4500 | nM | CHEMBL_ACT_15606669 |
| HTR2A | 5.35 | AC50 | 4432 | nM | CHEMBL_ACT_25173653 |
| CYP3A4 | 5.3 | Potency | 5012 | nM | CHEMBL_ACT_4993868 |
| CYP3A4 | 5.3 | Potency | 5012 | nM | CHEMBL_ACT_5059011 |
| P22906 | 5.3 | IC50 | 5000 | nM | CHEMBL_ACT_515174 |
Target pathways
Aggregated over 2 target gene(s): SLC47A1, SLC47A2.
Top Reactome pathways
4 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Transport of small molecules | 2 | SLC47A1, SLC47A2 |
| R-HSA-425366 | 2 | SLC47A1, SLC47A2 |
| SLC-mediated transmembrane transport | 2 | SLC47A1, SLC47A2 |
| SLC-mediated transport of organic cations | 2 | SLC47A1, SLC47A2 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| obsolete organic cation transport | 2 |
| transmembrane transport | 2 |
| xenobiotic detoxification by transmembrane export across the plasma membrane | 2 |
| proton transmembrane transport | 2 |
| xenobiotic transmembrane transport | 1 |
| putrescine transport | 1 |
| xenobiotic transport | 1 |
| amino acid import across plasma membrane | 1 |
| L-arginine import across plasma membrane | 1 |
| L-alpha-amino acid transmembrane transport | 1 |
| thiamine transmembrane transport | 1 |
| monoatomic cation transmembrane transport | 1 |
| L-arginine transmembrane transport | 1 |
Indications & clinical
Indications
2 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).
| Indication | Phase | MONDO | EFO |
|---|---|---|---|
| malaria | 4 | MONDO:0005136 | EFO:0001068 |
| toxoplasmosis | 4 | MONDO:0005989 | EFO:0007517 |
16 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.
| Disease (in trials) | Phase | MONDO | EFO |
|---|---|---|---|
| anemia | 3 | MONDO:0002280 | EFO:0004272 |
| congenital toxoplasmosis | 3 | MONDO:0005715 | EFO:0007220 |
| Plasmodium falciparum malaria | 3 | MONDO:0005920 | EFO:0007444 |
| Plasmodium vivax malaria | 3 | MONDO:0005921 | EFO:0007445 |
| schistosomiasis | 3 | MONDO:0015254 | EFO:1001475 |
| HIV infectious disease | 3 | MONDO:0005109 | EFO:0000180 |
| pneumocystosis | 3 | MONDO:0019121 | EFO:0007448 |
| chorioretinitis | 3 | MONDO:0004674 | HP:0012424 |
| depressive disorder | 3 | MONDO:0002050 | MONDO:0002050 |
| cerebral toxoplasmosis | 2 | MONDO:0005697 | EFO:0007200 |
| familial amyotrophic lateral sclerosis | 1 | MONDO:0005144 | EFO:0001356 |
| B-cell chronic lymphocytic leukemia | 1 | MONDO:0004948 | EFO:0000095 |
| myelodysplastic syndrome | 1 | MONDO:0018881 | EFO:0000198 |
| Sandhoff disease | 1 | MONDO:0010006 | MONDO:0010006 |
| Tay-Sachs disease | 1 | MONDO:0010100 | MONDO:0010100 |
| GM2 gangliosidosis | 1 | MONDO:0017720 | MONDO:0017720 |
4 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 51.
Phase distribution
| Phase | Trials |
|---|---|
| Not specified | 14 |
| PHASE3 | 11 |
| PHASE1 | 10 |
| PHASE4 | 6 |
| PHASE1/PHASE2 | 6 |
| PHASE2 | 2 |
| PHASE2/PHASE3 | 1 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00004317 | PHASE4 | RECRUITING | Pyrimethamine, Sulfadiazine, and Leucovorin in Treating Patients With Congenital Toxoplasmosis |
| NCT00125489 | PHASE4 | COMPLETED | CQSP in Malawi: Chloroquine and Sulfadoxine-pyrimethamine Efficacy for the Treatment of Malaria in Malawi |
| NCT00164255 | PHASE4 | COMPLETED | Efficacy of Combination Therapy for Prevention of Effects of Malaria During Pregnancy |
| NCT00453856 | PHASE4 | TERMINATED | Efficacy of Sulfadoxine-Pyrimethamine for Treating Malaria in Gabonese Children |
| NCT05478954 | PHASE4 | UNKNOWN | Chemoprevention Efficacy Study in Burkina Faso |
| NCT05980156 | PHASE4 | COMPLETED | Comparing Chemoprevention Drugs for School-based Malaria Control |
| NCT00000727 | PHASE3 | COMPLETED | A Controlled Comparative Trial of Sulfamethoxazole-Trimethoprim Versus Aerosolized Pentamidine for Secondary Prophylaxis of Pneumocystis Carinii Pneumonia in AIDS Patients Receiving Azidothymidine (AZT) |
| NCT00123552 | PHASE3 | COMPLETED | Longitudinal Antimalarial Combinations in Uganda |
| NCT00132548 | PHASE3 | COMPLETED | A Trial of Four Drug Regimens for the Prevention of Malaria in Senegalese Children |
| NCT00146718 | PHASE2/PHASE3 | COMPLETED | Anti-Malarial Drug Resistance in Cameroon |
| NCT00299247 | PHASE3 | WITHDRAWN | SP Resistance and Falciparum Malaria Transmission |
| NCT00300404 | PHASE3 | COMPLETED | Effect of Specific Anti-Toxoplasmatic Add-on Medication in Toxoplasma Gondii Seropositive Individuals With Schizophrenia or Major Depression |
| NCT00361114 | PHASE3 | TERMINATED | IPT and Efficacy of Sulphadoxine/Pyrimethamine and Chlorproguanil/Dapsone in 6-59 Month Old Children With Malaria. |
| NCT00399074 | PHASE3 | COMPLETED | Sulfadoxine- Pyrimethamine Versus Weekly Chloroquine for Malaria Prevention in Children With Sickle Cell Anemia |
| NCT01054651 | PHASE3 | COMPLETED | A Randomised Trial of Artesunate-sulfamethoxypyrazine/Pyrimethamine Versus Praziquantel for the Treatment of S. Mansoni |
| NCT01189448 | PHASE3 | COMPLETED | Prevention of Congenital Toxoplasmosis With Pyrimethamine + Sulfadiazine Versus Spiramycine During Pregnancy |
| NCT04783051 | PHASE3 | COMPLETED | Comparison of ISTp- PYRAMAX-US-RDT to IPTp-SP to Prevent Malaria in Pregnant Women in DRC (ULTRAPYRAPREG) |
| NCT05471544 | PHASE3 | UNKNOWN | Effectiveness, Feasibility and Acceptability of Seasonal Malaria Chemoprevention in Aweil South County in South Sudan |
| NCT07384624 | PHASE1/PHASE2 | NOT_YET_RECRUITING | Combining Latency Reversing Agents to Address the HIV Reservoir |
| NCT00000643 | PHASE2 | COMPLETED | Primary Prophylaxis of Cerebral Toxoplasmosis in HIV-Infected Patients |
| NCT00000794 | PHASE2 | COMPLETED | Phase II Randomized Open-Label Trial of Atovaquone Plus Pyrimethamine and Atovaquone Plus Sulfadiazine for the Treatment of Acute Toxoplasmic Encephalitis |
| NCT01066663 | PHASE1/PHASE2 | COMPLETED | Pyrimethamine for the Treatment of Relapsed Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma |
| NCT01083667 | PHASE1/PHASE2 | COMPLETED | SOD1 Inhibition by Pyrimethamine in Familial Amyotrophic Lateral Sclerosis (ALS) |
| NCT01102686 | PHASE1/PHASE2 | COMPLETED | Pyrimethamine as a Treatment for Late-Onset GM2-gangliosidosis (Tay-Sachs and Sandhoff Disease) |
| NCT03525730 | PHASE1/PHASE2 | COMPLETED | LRAs United as a Novel Anti-HIV Strategy. |
| NCT03952650 | PHASE1/PHASE2 | COMPLETED | Sanaria PfSPZ Challenge With Pyrimethamine or Chloroquine Chemoprophylaxis Vaccination (PfSPZ-CVac Approach): A Randomized Double Blind Placebo Controlled Phase I/II Trial to Determine Safety and Protective Efficacy Against Natural Plasmodium Falcipa… |
| NCT00000966 | PHASE1 | COMPLETED | A Study of Azithromycin Plus Pyrimethamine in the Treatment of a Brain Infection in Patients With AIDS |
| NCT00000973 | PHASE1 | COMPLETED | A Study of Pyrimethamine in the Treatment of Infection by a Certain Parasite in HIV-Positive Patients |
| NCT00065390 | PHASE1 | COMPLETED | Pyrimethamine to Treat Autoimmune Lymphoproliferative Syndrome |
| NCT00679744 | PHASE1 | WITHDRAWN | A Phase I Study of Pyrimethamine in Patients With GM2 Gangliosidosis |
| NCT01973933 | PHASE1 | COMPLETED | Clinical Trial to Investigate the Pharmacokinetic/Pharmacodynamic Drug-Drug Interaction of Pyrimethamine and Metformin IR |
| NCT02511054 | PHASE1 | COMPLETED | Sanaria PfSPZ Challenge With Pyrimethamine Chemoprophylaxis (PfSPZ-CVac Approach): Phase 1 Trial to Determine Safety and Protective Efficacy of Sanaria PfSPZ Challenge With Concurrent Pyrimethamine Treatment That Inhibits Development of Asexual B… |
| NCT03057990 | PHASE1 | WITHDRAWN | Pyrimethamine for Intermediate/High-risk Myelodysplastic Syndromes (MDS) |
| NCT03083847 | PHASE1 | COMPLETED | Dose Escalation PfSPZ-CVac |
| NCT03258762 | PHASE1 | COMPLETED | Phase I Study of Pyrimethamine in Healthy Japanese and Caucasian Subjects |
| NCT04086719 | PHASE1 | COMPLETED | An Investigational Study to Determine the Drug Level Profile of BMS-986165 in Healthy Male Volunteers Following Transporter Inhibition. |
| NCT05678348 | EARLY_PHASE1 | COMPLETED | Pyrimethamine as an Inhibitor of NRF2 in HPV-unrelated Locally Advanced Head and Neck Squamous Cell Carcinoma |
| NCT05856357 | Not specified | ACTIVE_NOT_RECRUITING | Perennial Malaria Chemoprevention (PMC) in Côte D’Ivoire |
| NCT05889052 | Not specified | ACTIVE_NOT_RECRUITING | Perennial Malaria Chemoprevention (PMC) in Cameroon |
| NCT05949190 | Not specified | ACTIVE_NOT_RECRUITING | Improving Cognition and Gestational Duration With Targeted Nutrition |
| NCT00000666 | Not specified | COMPLETED | A Randomized Prospective Study of Pyrimethamine Therapy for Prevention of Toxoplasmic Encephalitis in HIV-Infected Individuals With Serologic Evidence of Latent Toxoplasma Gondii Infection |
| NCT00000674 | Not specified | COMPLETED | A Pilot Study of Oral Clindamycin and Pyrimethamine for the Treatment of Toxoplasmic Encephalitis in Patients With AIDS |
| NCT00002064 | Not specified | COMPLETED | Toxoplasmic Encephalitis in Patients With AIDS. Treatment and Prevention of Relapse |
| NCT00126906 | Not specified | COMPLETED | Prevention of Malaria During Pregnancy Using Intermittent Preventive Treatment With Sulfadoxine-Pyrimethamine: Malawi |
| NCT00304980 | Not specified | TERMINATED | Comparative Evaluation of the Safety and the Efficacy of 2 Antimalarials Depending on HIV Status |
| NCT00766662 | Not specified | COMPLETED | Intermittent Preventive Treatment in Infant in Mali |
| NCT00951106 | Not specified | COMPLETED | Therapeutic Efficacy Study of Pyrimethamine/Sulfdoxine (Fansidar®) for the Treatment of Uncomplicated Falciparum Malaria in the Peruvian Amazon |
| NCT03454048 | Not specified | COMPLETED | Controlled Human Malaria Infection Model for Evaluation of Transmission-blocking Interventions - Study 2 |
| NCT03944317 | Not specified | UNKNOWN | Azithromycin (AZ) and Sulphadoxine-pyrimethamine (SP) for Malaria Prevention in Pregnant Women (IPT-AZ/IPT-SP) |
| NCT05354258 | Not specified | UNKNOWN | Feasibility and Safety of Combining Anti-malarial With Deworming Drugs in African Children |
| NCT06002438 | Not specified | COMPLETED | Eggs for Gut Health |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 2 clinical and 7 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
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.
69 molecules share ≥1 primary target. Top 69 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| BUSPIRONE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| CARVEDILOL | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| CHLORHEXIDINE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| CIMETIDINE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| DIHYDROERGOTAMINE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| DIPYRIDAMOLE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| DISOPYRAMIDE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| DOMPERIDONE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| EPINASTINE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| ETHINYL ESTRADIOL | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| FAMOTIDINE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| IMATINIB | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| IMIPRAMINE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| IRINOTECAN | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| MITOXANTRONE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| ONDANSETRON | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| ORPHENADRINE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| PANTOPRAZOLE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| PENTAMIDINE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| PRAZOSIN | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| QUINIDINE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| RIMANTADINE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| RISPERIDONE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| RITONAVIR | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| TOPOTECAN | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| TUBOCURARINE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| VECURONIUM BROMIDE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| ZAFIRLUKAST | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1, SLC47A2 |
| BITHIONOL | ChEMBL | Phase 4 (approved) | SLC47A1, SLC47A2 |
| DABIGATRAN | ChEMBL + PubChem | Phase 3 (approved) | SLC47A1, SLC47A2 |
| CAMOSTAT | ChEMBL | Phase 3 | SLC47A1, SLC47A2 |
| GABEXATE | ChEMBL | Phase 3 | SLC47A1, SLC47A2 |
| INDINAVIR | ChEMBL | Phase 3 | SLC47A1, SLC47A2 |
| NIFEKALANT | ChEMBL | Phase 3 | SLC47A1, SLC47A2 |
| Aripiprazole | PubChem | Approved | SLC47A1, SLC47A2 |
| Metformin | PubChem | Approved | SLC47A1, SLC47A2 |
| Pimozide | PubChem | Approved | SLC47A1, SLC47A2 |
| AMANTADINE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1 |
| CLONIDINE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1 |
| SPIRONOLACTONE | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1 |
| SUMATRIPTAN | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1 |
| TELMISARTAN | ChEMBL + PubChem | Phase 4 (approved) | SLC47A1 |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | SLC47A1 |
| GRANISETRON | ChEMBL | Phase 4 (approved) | SLC47A1 |
| LEVOFLOXACIN | ChEMBL | Phase 4 (approved) | SLC47A1 |
| MARAVIROC | ChEMBL | Phase 4 (approved) | SLC47A1 |
| NOSCAPINE | ChEMBL | Phase 4 (approved) | SLC47A1 |
| RANITIDINE | ChEMBL | Phase 4 (approved) | SLC47A1 |
| TACRINE | ChEMBL | Phase 4 (approved) | SLC47A1 |
| CORTISONE | ChEMBL + PubChem | Phase 3 (approved) | SLC47A1 |
| AFIMETORAN | ChEMBL | Phase 2 | SLC47A2 |
| azacitidine | PubChem | Approved | SLC47A1 |
| Cetirizine | PubChem | Approved | SLC47A1 |
| Ciclopirox | PubChem | Approved | SLC47A1 |
| Dexamethasone | PubChem | Approved | SLC47A1 |
| Diclofenac | PubChem | Approved | SLC47A1 |
| Enalapril | PubChem | Approved | SLC47A1 |
| Erythromycin | PubChem | Approved | SLC47A1 |
| Furosemide | PubChem | Approved | SLC47A1 |
| Indomethacin | PubChem | Approved | SLC47A1 |
| Irbesartan | PubChem | Approved | SLC47A1 |
| Lidocaine | PubChem | Approved | SLC47A1 |
| Losartan | PubChem | Approved | SLC47A1 |
| methylergonovine | PubChem | Approved | SLC47A1 |
| niacin | PubChem | Approved | SLC47A1 |
| Pramipexole | PubChem | Approved | SLC47A2 |
| Procainamide | PubChem | Approved | SLC47A1 |
| Sulfacetamide | PubChem | Approved | SLC47A1 |
| Thiabendazole | PubChem | Approved | SLC47A1 |
Related Atlas pages
- Genes: SLC47A1, SLC47A2
- Indicated for: malaria, toxoplasmosis
- In clinical trials for: anemia, congenital toxoplasmosis, Plasmodium falciparum malaria, Plasmodium vivax malaria, schistosomiasis, HIV infectious disease, pneumocystosis, chorioretinitis, depressive disorder, cerebral toxoplasmosis
- Drugs: Buspirone, Carvedilol, Chlorhexidine, Cimetidine, Dihydroergotamine, Dipyridamole, Disopyramide, Domperidone, Epinastine, Ethinyl Estradiol, Famotidine, Imatinib, Imipramine, Irinotecan, Mitoxantrone, Ondansetron, Orphenadrine, Pantoprazole, Pentamidine, Prazosin, Quinidine, Rimantadine, Risperidone, Ritonavir, Topotecan, Tubocurarine, Vecuronium Bromide, Zafirlukast, Bithionol, Dabigatran, Camostat, Gabexate, Nifekalant, Aripiprazole, Metformin, Pimozide, Amantadine, Clonidine, Spironolactone, Sumatriptan, Telmisartan, Astemizole, Granisetron, Levofloxacin, Maraviroc, Noscapine, Ranitidine, Tacrine, Cortisone, azacitidine, Cetirizine, Ciclopirox, Dexamethasone, Diclofenac, Enalapril, Erythromycin, Furosemide, Indomethacin, Irbesartan, Lidocaine, Losartan, methylergonovine, niacin, Pramipexole, Procainamide, Sulfacetamide, Thiabendazole