S.N. | Drugs | Marketing authotization and commercial product | Cure rate | Mechanism of action | Advantages | Limitations |
---|---|---|---|---|---|---|
1 | Pentavalent antimonials | Albert David, India (generic SSG); Wellcome (Pentostam); Sanofi Aventis (Glucantime) | 39–95 % depending on geographical condition (50 % in Bihar) | Act as prodrug, inhibit trypanothione reductase, increase the ROS | Low cost and easy available | Parasite resistance especially in India, cardiotoxic, 30 day iv/im treatment in hospital, painful injections |
Inhibit macromolecular biosynthesis in amastigotes | ||||||
2 | Amphotericin B | Life care, India | >98 % in all regions | Form complexes with sterols mainly ergosterols of parasite membrane leading to increase permeability resulting in cell death | High efficacy, 1st line treatment in case of antimonial resistance | Dose-limiting renal toxicity, 15–30 day slow iv infusion treatment over 4–6h in hospital, hypokalaemia |
(Fungitericin); Bristol –Myers (Fungisone) | ||||||
3 | Liposomal amphotericin B | Gilead (AmBisome); | >98Â % | Targeted delivery of drug to infected macrophages and kill the parasites as AmB | Highest therapeutic index of available VL drugs, No need of hospitalization, substantially less nephro-toxic than AmB | Expensive, requirement of cool chain temperature maintainance |
Lifecare Innovation (Fungisome); Bharat Serum and Vaccine (Amphomul); | ||||||
Sequus Pharmaceuticals (Amphocil); | ||||||
ENZON Pharmaceuticals (Abelcet); | ||||||
Lifecare Innovation (Kalsome) | ||||||
4 | Miltefosine | Paladin Labs (Impavido) | 94–97 % | Modulate cell surface receptors and inositol metabolism of parasites, and cell death is mediated by apoptosis, Inhibit the cytochrome C oxidase | Oral drug, Safe in HIV-VL co-infection | Teratogenic in experimental animals, originally developed as an anti- cancer drug, expensive, GI toxicity, hepato- & renaltoxicity in phase-4 |
5 | Paromomycin | Gland Pharma/iOWH | 94Â % (India) | Binds to 30S ribosomal subunit and interfere with protein biosynthesis, decrease the membrane potential of parasite | Cheapest drug | An aminoglycoside, therefore nephro- and ototoxicity possible, but have not been reported in VL patients, although reversible high tone audiometric shift may occasionally occur during treatment |
6 | Pentamidine | Sanofi Aventis (Pentacarinat) | 70–80 % | Inhibit mitochondrial topoisomerase II and inhibit the transcription process | Effective in combination therapy | Gastointestinal adverse effect, hypotension, diabetes mellitus |