Trimetrexate

ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS

Key facts

Trimetrexate is an ofm drug catalogued in DrugCentral. It was first approved by the FDA in 1993. DrugCentral lists 13 molecular targets, including Dhfr, Dihydrofolate reductase and DHFR. Recorded indications include Pneumocystosis jiroveci pneumonia.

• Approval status: ofm (first approved 1993 by the FDA).
• Molecular targets: Dhfr, Dihydrofolate reductase, DHFR and folA (13 listed in DrugCentral).
• Indications: Pneumocystosis jiroveci pneumonia.
• ATC code: P01AX07 (Other agents against amoebiasis and other protozoal diseases).
• Molecular formula: C19H23N5O3; molecular weight 369.43 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Pneumocystosis jiroveci pneumonia

Contraindications (5)

• Bone marrow depression
• Breastfeeding (mother)
• Disease of liver
• Kidney disease
• Pregnancy, function

Mechanism & targets

Molecular targets (13)

Target	Gene	Action	Activity
Dihydrofolate reductase	Dhfr	unknown	Ki 10.22
Dihydrofolate reductase	—	inhibitor	Ki 9.15
Dihydrofolate reductase	DHFR	unknown	Ki 8.85
Dihydrofolate reductase	folA	unknown	IC50 8.82
Dihydrofolate reductase	DFR1	unknown	Ki 8.72
Dihydrofolate reductase	Dhfr	unknown	IC50 8.52
Bifunctional dihydrofolate reductase-thymidylate synthase	—	unknown	IC50 8.29
Bifunctional dihydrofolate reductase-thymidylate synthase	—	unknown	Ki 8.18
Dihydrofolate reductase	dfrA17	unknown	IC50 8.15
Dihydrofolate reductase	folA	unknown	IC50 8.00
Dihydrofolate reductase	folA	unknown	IC50 7.57
Dihydrofolate reductase	DFR1	unknown	IC50 7.38
Folylpolyglutamate synthase, mitochondrial	FPGS	unknown	—

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1993-12-17	FDA	—	—

ATC classification

ATC code	Therapeutic hierarchy
P01AX07	ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS › ANTIPROTOZOALS › AGENTS AGAINST AMOEBIASIS AND OTHER PROTOZOAL DISEASES › Other agents against amoebiasis and other protozoal diseases

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Trimetrexate is on its molecule page.

• Molecular formula: C₁₉H₂₃N₅O₃
• Molecular weight: 369.43 g/mol
• CAS number: 52128-35-5
• InChIKey: NOYPYLRCIDNJJB-UHFFFAOYSA-N
• PubChem CID: 5583

COC1=CC(NCC2=CC=C3N=C(N)N=C(N)C3=C2C)=CC(OC)=C1OC

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Trimetrexate used for?

DrugCentral lists the following indications for Trimetrexate: Pneumocystosis jiroveci pneumonia.

How does Trimetrexate work?

Its molecular targets in DrugCentral include Dhfr, Dihydrofolate reductase (inhibitor), DHFR and folA.

When was Trimetrexate first approved?

Trimetrexate was first approved by the FDA in 1993.

What is the chemical formula of Trimetrexate?

Trimetrexate has the molecular formula C19H23N5O3 and a molecular weight of 369.43 g/mol.

Sources

• DrugCentral drug card 2757 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL119 — compound record and bioactivity
• PubChem CID 5583 — chemical identifiers
• DrugBank DB01157 — drug record
• FDA UNII UPN4ITI8T4 — substance identity
• DailyMed: FDA labels for Trimetrexate — current prescribing information (label search)
• UniProt P00374 (DHFR) — target protein
• UniProt Q05932 (FPGS) — target protein

How this page is built: methodology · editorial policy & corrections.