proguanil Report issue

Small molecule Approved FDA Priority Review FDA
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Active Ingredient History

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Proguanil is a prophylactic antimalarial drug, which works by stopping the malaria parasite, Plasmodium falciparum and Plasmodium vivax, from reproducing once it is in the red blood cells. Proguanil in combination with atovaquone are marked under the brand name malarone, which is indicated for the treatment of acute, uncomplicated P. falciparum malaria and for the prophylaxis of Plasmodium falciparum malaria, including in areas where chloroquine resistance has been reported. Atovaquone and proguanil, interfere with 2 different pathways involved in the biosynthesis of pyrimidines required for nucleic acid replication. Atovaquone is a selective inhibitor of parasite mitochondrial electron transport. Proguanil hydrochloride primarily exerts its effect by means of the metabolite cycloguanil, a dihydrofolate reductase inhibitor. Inhibition of dihydrofolate reductase in the malaria parasite disrupts deoxythymidylate synthesis. Recently were done experiments, which confirmed the hypothesis that proguanil might act on another target than dihydrofolate reductase. In addition, was made conclusion, that effectiveness of malarone was due to the synergism between atovaquone and proguanil and may not require the presence of cycloguanil.   NCATS

Chemistry

More Chemistry

Pharmacology

Combination drugs

( atovaquone (mepron), proguanil - other name: malarone )

Alternative names

1-(p-chlorophenyl)-5-isopropylbiguanide | 336u50 | amosene | atovaquone and proguanil | bamate | chlorguanide | chloroguanide | chloroguanide hcl | chloroguanide hydrochloride | gwah7673a | n-(4-chlorophenyl)-n'-(isopropyl)-imidodicarbonimidic diamide | paludrine | proguanil | proguanil chloride | proguanil hcl | proguanil hydrochloride | proguanilum | proquanil

Organizations (39)

Research & Development (37)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (3)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (10)

Approved Indications (2)


 

Malaria

Malaria, Falciparum (approved 2000)

Experimental Indications - Clinical Trial Phases 1-4 (10)


 

Anemia, Sickle Cell (Phase 1/Phase 2)

Biological Availability (Phase 1)

Cytochrome P-450 CYP2C19 (Phase 1)

Gastroesophageal Reflux (Phase 1)

HIV Infections (Phase 4)

Malaria ()

Malaria, Falciparum (Phase 4)

Metabolism (Phase 1)

Rabies (Phase 4)

Sports Medicine (Phase 1)

Overview

  • Highest Phase: Phase 4
  • # of Trials: 28
  • # of Trial Organizations: 37

Trials by Phase

Trial Phase Start Date Organizations Indications

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