Trimetrexate
Trimetrexate is a lipophilic antifolate that inhibits dihydrofolate reductase (DHFR), blocking tetrahydrofolate synthesis required for DNA replication, thereby exerting cytotoxic effects on rapidly dividing cells. It was used as an alternative treatment for Pneumocystis jirovecii pneumonia in immunocompromised patients and investigated as an antineoplastic agent in colorectal cancer and leukemia. It requires leucovorin rescue to protect normal host cells.
分子量
369.4000 g/mol
LogP
2.50
TPSA
118.00 Ų
Lipinski 五规则
符合
治疗领域
Pharmacokinetics (PK)
Pharmacodynamics (PD)
二维结构
Cite this structure
Embed this structure
SMILES
COc1cc(NCc2ccc3nc(N)nc(N)c3c2C)cc(OC)c1OC
InChI
InChI=1S/C19H23N5O3/c1-10-11(5-6-13-16(10)18(20)24-19(21)23-13)9-22-12-7-14(25-2)17(27-4)15(8-12)26-3/h5-8,22H,9H2,1-4H3,(H4,20,21,23,24)
Molecular Formula
C19H23N5O3
HBD / HBA
3 / 8
可旋转键数
6
重原子数
27
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
常见问题
Trimetrexate is a lipophilic antifolate that inhibits dihydrofolate reductase (DHFR), blocking tetrahydrofolate synthesis required for DNA replication, thereby exerting cytotoxic effects on rapidly dividing cells. It was used as an alternative treatment for Pneumocystis jirovecii pneumonia in immunocompromised patients and investigated as an antineoplastic agent in colorectal cancer and leukemia. It requires leucovorin rescue to protect normal host cells.
Yes, Trimetrexate is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL119. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 5583. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.
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