Lonidamine Derivatives
Gamendazole, H2-Gamendazole, Adjudin, BHD
- User: Male
- Hormonal: Non-Hormonal
-
Delivery type:
- Not Yet Determined
-
Intended Duration:
- Not Yet Determined
- Development Stage: Pre-Clinical
- Developer(s)/researcher(s): University of Kansas Medical Center, University of Minnesota, Nantong University
Details
- API: Gamendazole/Adjudin/BHD
- Target: Sertoli Cells
-
Mechanism of Action:
- Not Yet Determined
- Inactive Materials: Not Yet Determined
- Regimen: Not Yet Determined
- MPT: Not Potential MPT
- Promising Attributes: Lonidamine is known to have a strong anti-spermatogenesis effect, making it a desirable option for further development. The irreversibility and toxicity of its derivatives, however, may impede use in human subjects.
Product Status
Active/Recent Pre-Clinical Development
History
See linked literature below for information on safety and biocompatibility
Investigation on the use of lonidamine, a derivative of indazole-3-carboxylic acid, and lonidamine derivatives for male contraception began in 1979 and has been steady through 2023. The derivatives gamendazole and adjudin have emerged as the most viable drug candidates; both, however, have undesirable toxicology and reversibility profiles. Refinement of these derivatives is active as of 2022. 2023 bench and animal research from Nantong University suggests the viability of a new derivative, BHD, as a less-toxic alternative.
Publications
doi: 10.1159/000238040
doi: 10.1159/000238043
doi: 10.1159/000238050
doi: 10.1007/978-3-642-68511-8_35
doi: 10.1093/oxfordjournals.humrep.a138637
doi: 10.1095/biolreprod65.2.449
doi: 10.1095/biolreprod.106.057810
doi: 10.1530/REP-10-0464
doi: 10.1371/journal.pone.0060656
doi: 10.1124/jpet.122.001195
doi: 10.1021/acsomega.3c01840