ALDH1a2 Inhibitors

Alternative Name: Inhibitors of Testicular Retinoic Acid Biosynthesis

Description: ALDH1A2 is an enzyme involved in testicular retinoic acid biosynthesis, that if blocked can arrest spermotogenesis. Small molecule inhibitors of ALDH1A2 are being developed as long-term oral, reversible male contraceptives, based on earlier work on bisdichloroacetyldiamines (BDADs).

Product Details

User: Male

Hormonal: No

Delivery Method: Oral

Duration Type: Long-acting

Duration: Months to years

Regimen:
  • daily

Active Pharmaceutical Ingredient (API):
  • ALDH1A2 inhibitors

Multipurpose Preventive Technology (MPT): No

Status Details

Developer: University of Washington, University of Minnesota

Project Phase: Pre-Clinical and Clinical Development

Development Stage: Pre-clinical

Active Development: Yes

Status Details:
  • Currently conducting preclinical, in vitro, and early-phase animal testing.
  • Study on ALDH1a2 mechanism of action published in 2018.

Additional Information

References:
  • Paik J, et al. (2014) Inhibition of Retinoic Acid Biosynthesis by the Bisdichloroacetyldiamine WIN 18,446 Markedly Suppresses Spermatogenesis and Alters Retinoid Metabolism in Mice. The Journal of Biological Chemistry. 289(21):15104-15117.

  • Chen Y, et al. (2018). Structural Basis of ALDH1A2 Inhibition by Irreversible and Reversible Small Molecule Inhibitors.​ ACS Chem Biol. 13(3):582-590.

Footnotes:
  • See entry on Bisdichloroacetyldiamines (BDADs).

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