H2-Gamendazole
Alternative Name: H2-GMZ
Description: H2-Gamendazole rapidly acts via Sertoli cells by inducing a transient increase in interleukin 1A causing disruption of spermatid-Sertoli cell junctions. There is premature release of spermatids, which results in semen without sperm. Gamendazole, along with Adjudin, are derivatives of lonidamine.
Product Details
Active Pharmaceutical Ingredient (API):
Status Details
Developer: ,
Status Details: - Contraceptive activity proven in rats after single oral dose in 3-6mg/kg range.
- High oral bioavailability. Identical blockage of late stage spermatogenesis proven in mice and rabbits.
- No-side effects observed to-date. Reversibility of infertility with multiple low dose regimens in rats and other species needs to be investigated.
- First non-human primate pilot study started in 2010, looking at initial safety and proof of concept based on semen sperm count. Non-GLP pre-clinical toxicology (MTD, 7-day TOX, Toxicokinetics) also starting in 2010.
- Contraceptive activity proven in rats after single oral dose in 3-6mg/kg range.
- High oral bioavailability. Identical blockage of late stage spermatogenesis proven in mice and rabbits.
- No-side effects observed to-date. Reversibility of infertility with multiple low dose regimens in rats and other species needs to be investigated.
- First non-human primate pilot study started in 2010, looking at initial safety and proof of concept based on semen sperm count. Non-GLP pre-clinical toxicology (MTD, 7-day TOX, Toxicokinetics) also starting in 2010.
Additional Information
References: Tash JS, et al. (2008) A novel potent indazole carboxylic acid derivative blocks spermatogenesis in rats after a single oral dose and Is contraceptive. Biol Reprod. 78:1127-1138.
Tash JS et al. (2008) Gamendazole, an orally active indazole carboxylic acid male contraceptive agent, targets HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A), and stimulates II1a transcription in rat Sertoli cells. Biol Reprod. 78:1139-1152.
Holets L, et al. (2011). Effect of H2-Gamendazole and Other Indazole Carboxylic Acid (ICA) Analogs on Primary Rat Sertoli Cells Cytoskeletal Structure and Elongation Factor 1 Alpha (EEF1A1) Expression and Function. Biology of reproduction. 85:1, 582-583.
Tash JS, et al. (2008) A novel potent indazole carboxylic acid derivative blocks spermatogenesis in rats after a single oral dose and Is contraceptive. Biol Reprod. 78:1127-1138.
Tash JS et al. (2008) Gamendazole, an orally active indazole carboxylic acid male contraceptive agent, targets HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A), and stimulates II1a transcription in rat Sertoli cells. Biol Reprod. 78:1139-1152.
Holets L, et al. (2011). Effect of H2-Gamendazole and Other Indazole Carboxylic Acid (ICA) Analogs on Primary Rat Sertoli Cells Cytoskeletal Structure and Elongation Factor 1 Alpha (EEF1A1) Expression and Function. Biology of reproduction. 85:1, 582-583.