Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C14H12F7N5S |
| Molecular Weight | 415.332 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=NC2=NC(=NN2C(NC3=CC=C(C=C3)S(F)(F)(F)(F)F)=C1)C(C)(F)F
InChI
InChIKey=OIZSVTOIBNSVOS-UHFFFAOYSA-N
InChI=1S/C14H12F7N5S/c1-8-7-11(26-13(22-8)24-12(25-26)14(2,15)16)23-9-3-5-10(6-4-9)27(17,18,19,20)21/h3-7,23H,1-2H3
DSM265 is an experimental antimalarial that selectively inhibits the parasite dihydroorotate dehydrogenase (DHODH). DSM265 is the first DHODH inhibitor to reach clinical development for treatment of malaria. DSM265 is highly selective toward DHODH of the malaria parasite Plasmodium, efficacious against both blood and liver stages of P. falciparum, and active against drug-resistant parasite isolates. The only possible DSM265-related adverse event was a moderate transient elevation in serum bilirubin.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| DSM265 at 400 Milligrams Clears Asexual Stage Parasites but Not Mature Gametocytes from the Blood of Healthy Subjects Experimentally Infected with Plasmodium falciparum. | 2019-04 |
|
| Identification and Mechanistic Understanding of Dihydroorotate Dehydrogenase Point Mutations in Plasmodium falciparum that Confer in Vitro Resistance to the Clinical Candidate DSM265. | 2019-01-11 |
|
| DSM265: a novel drug for single-dose cure of Plasmodium falciparum malaria. | 2018-08 |
|
| Antimalarial activity of single-dose DSM265, a novel plasmodium dihydroorotate dehydrogenase inhibitor, in patients with uncomplicated Plasmodium falciparum or Plasmodium vivax malaria infection: a proof-of-concept, open-label, phase 2a study. | 2018-08 |
|
| A Randomized Trial Evaluating the Prophylactic Activity of DSM265 Against Preerythrocytic Plasmodium falciparum Infection During Controlled Human Malarial Infection by Mosquito Bites and Direct Venous Inoculation. | 2018-02-14 |
|
| DSM265 for Plasmodium falciparum chemoprophylaxis: a randomised, double blinded, phase 1 trial with controlled human malaria infection. | 2017-06 |
|
| Safety, tolerability, pharmacokinetics, and activity of the novel long-acting antimalarial DSM265: a two-part first-in-human phase 1a/1b randomised study. | 2017-06 |
|
| A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria. | 2015-07-15 |
|
| Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential. | 2011-08-11 |
Patents
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Common Name | English | ||
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Preferred Name | English | ||
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Systematic Name | English | ||
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Systematic Name | English |
| Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
598417
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300000052922
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DB12397
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ACTIVE MOIETY
