Investigational Drug Details
| Drug ID: | D124 |
| Drug Name: | Trimethoprim |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB00440 |
| DrugBank Description: | Trimethoprim is a pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to pyrimethamine. The interference with folic acid metabolism may cause a depression of hematopoiesis. It is potentiated by sulfonamides and the trimethoprim-sulfamethoxazole combination is the form most often used. It is sometimes used alone as an antimalarial. Trimethoprim resistance has been reported. |
| PubChem ID: | 5578 |
| CasNo: | 738-70-5 |
| Repositioning for NAFLD: | Yes |
| SMILES: | COC1=CC(CC2=CN=C(N)N=C2N)=CC(OC)=C1OC |
| Structure: |
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| InChiKey: | IEDVJHCEMCRBQM-UHFFFAOYSA-N |
| Molecular Weight: | 290.3177 |
| DrugBank Targets: | Dihydrofolate reductase |
| DrugBank MoA: | Trimethoprim inhibits dihydrofolate reductase. This inhibition prevents the conversion of dihydrofolic acid (DHF) to tetrahydrofolic acid (THF) in the thymidine synthesis pathway. Trimethoprim acts on bacterial dihydrofolate reductase with thousands of times the affinity of human dihydrofolate reductase. Sulfamethoxazole inhibits dihydrofolate synthetase (aka dihydropteroate synthetase), an enzyme involved further upstream in the same pathway. Trimethoprim and sulfamethoxazole are commonly used in combination due to their synergistic effects. This drug combination also reduces the development of resistance that is seen when either drug is used alone. |
| DrugBank Pharmacology: | Trimethoprim is a pyrimidine analogue that disrupts folate synthesis, an essential part of the thymidine synthesis pathway. Inhibition of the enzyme starves the bacteria of nucleotides necessary for DNA replication.The drug, therefore, exhibits bactericidal activity. |
| DrugBank Indication: | For the treatment of urinary tract infections, uncomplicated pyelonephritis (with sulfamethoxazole) and mild acute prostatitis. May be used as pericoital (with sulfamethoxazole) or continuous prophylaxis in females with recurrent cystitis. May be used as an alternative to treat asymptomatic bacteriuria during pregnancy (only before the last 6 weeks of pregnancy). Other uses include: alternative agent in respiratory tract infections (otitis, sinusitus, bronchitis and pneumonia), treatment of Pneumocystis jirovecii pneumonia (acute or prophylaxis), Nocardia infections, and traveller's diarrhea. |
| Targets: | |
| Therapeutic Category: | |
| Clinical Trial Progress: | |
| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L3300 | NCT00886366 | PHASE1 | TERMINATED | NO | 2009-04 | 2010-12-07 | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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| Article ID | PMID | Source | Title |
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