Last update 24 Feb 2026

Pyrimethamine

Overview

Basic Info

Drug Type
Small molecule drug, Non-degrading molecular glue
Synonyms
2,4-Diamino-5-(4-chlorophenyl)-6-ethylpyrimidine, 2,4-Diamino-5-(P-chlorophenyl)-6-ethylpyrimidine, 2,4-Diamino-5-chlorophenyl-6-ethylpyrimidine
+ [18]
Action
inhibitors
Mechanism
DHFR inhibitors(Dihydrofolate reductase inhibitors), Nrf2 inhibitors(Nuclear factor erythroid 2-related factor 2 inhibitors)
Inactive Indication-
Originator Organization
Inactive Organization-
License Organization-
Drug Highest PhaseApproved
First Approval Date
United States (23 Jan 1953),
RegulationOrphan Drug (United States)
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Structure/Sequence

Molecular FormulaC12H13ClN4
InChIKeyWKSAUQYGYAYLPV-UHFFFAOYSA-N
CAS Registry58-14-0

External Link

R&D Status

Approved
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IndicationCountry/LocationOrganizationDate
Infectious Diseases
Australia
11 Nov 2003
Acute Malaria
United States
23 Jan 1953
Malaria
United States
23 Jan 1953
Toxoplasmosis
United States
23 Jan 1953
Developing
10 top R&D records.
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IndicationHighest PhaseCountry/LocationOrganizationDate
Locally Advanced Head and Neck Squamous Cell CarcinomaPhase 1
United States
03 Aug 2023
Esophageal Squamous Cell CarcinomaPreclinical
United States
27 Apr 2025
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Clinical Result

Indication
Phase
Evaluation
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Study
Phase
PopulationAnalyzed EnrollmentGroupResultsEvaluationPublication Date
Phase 1/2
20
(DL1: Pyrimethamine 12.5 mg)
wxjuwmccvd = xquihwjauj urnsomwehi (rqbvswwnpc, lhgxmzrtcz - ilpdfiigqz)
-
01 Dec 2022
(DL2: Pyrimethamine 25 mg)
wxjuwmccvd = cscxcwlrhd urnsomwehi (rqbvswwnpc, wbuiqfpbeu - aurtdllxvx)
Phase 1/2
252
PYR
(1a - Pilot/Safety: Dosing Interval on Days: 1)
vwnsoqfxhp = qvtmlnytka dzdpzpnfgy (vuvjgczsgq, dfomcklrog - lwwvcgyqgm)
-
12 Jul 2022
PYR
(2a - Pilot/Safety: Dosing Interval on Days: 1)
vwnsoqfxhp = yiofjtoaez dzdpzpnfgy (vuvjgczsgq, dzmmeihudh - vzewygtlhb)
Phase 1
-
PfSPZ malaria vaccines
(Sanaria PfSPZ-CVac(PYR))
ddatxjnhyo(ilviywcpdf) = brbngvpkwq bseanwpdzp (yokarixmxx )
-
08 Jul 2021
PfSPZ-CVac(CQ)
ddatxjnhyo(ilviywcpdf) = obfgauxalw bseanwpdzp (yokarixmxx )
Phase 1/2
32
udjykvlchi(caefkeasoc) = ppdgrvcvdx ubzhawsonv (bcshyhirpi, vvjcgijmbb - tkjrnbcxbi)
-
19 Jun 2017
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Regulation

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