Repositioning Candidate Details

Candidate ID: R0259
Source ID: DB00738
Source Type: approved; investigational
Compound Type: small molecule
Compound Name: Pentamidine
Synonyms: 1,5-bis(4-amidinophenoxy)pentane; 4,4'-(1,5-pentanediylbis(oxy))bis-benzenecarboximidamide; 4,4'-(pentamethylenedioxy)dibenzamidine; 4,4'-Diamidinodiphenoxypentane; p,p'-(pentamethylenedioxy)dibenzamidine
Molecular Formula: C19H24N4O2
SMILES: NC(=N)C1=CC=C(OCCCCCOC2=CC=C(C=C2)C(N)=N)C=C1
Structure:
DrugBank Description: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of pneumocystis pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.
CAS Number: 100-33-4
Molecular Weight: 340.4195
DrugBank Indication: For the treatment of pneumonia due to <i>Pneumocystis carinii</i>.
DrugBank Pharmacology: Pentamidine is an antiprotozoal agent. It is an aromatic diamidine, and is known to have activity against <i>Pneumocystis carinii</i>. The exact nature of its antiprotozoal action is unknown. <i>in vitro</i> studies with mammalian tissues and the protozoan <i>Crithidia oncopelti</i> indicate that the drug interferes with nuclear metabolism producing inhibition of the synthesis of DNA, RNA, phospholipids and proteins. Little is known about the drug's pharmacokinetics. The medication is also useful in Leishmaniasis and in prophylaxis against sleeping sickness caused by <i>Trypanosoma brucei gambiense</i>. Hydration before treatment lessens the incidence and severity of side effects, which include liver or kidney dysfunction, hypertension, hypotension, hypoglycemia, hypocalemia, leukopenia, thrombcytopenia, anemia, and allergic reaction. It is generally well-tolerated.
DrugBank MoA: The mode of action of pentamidine is not fully understood. It is thought that the drug interferes with nuclear metabolism producing inhibition of the synthesis of DNA, RNA, phospholipids, and proteins.
Targets: DNA intercalation; tRNA (cytosine(38)-C(5))-methyltransferase other
Inclusion Criteria: Indication associated