Androgen receptor degrader

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A (selective) androgen receptor degrader or downregulator (SARD) is a type of drug which interacts with the androgen receptor (AR) such that it causes the AR to be degraded and thus downregulated. [1] They are under investigation for the treatment of prostate cancer and other androgen-dependent conditions. [1]

As of 2017, dimethylcurcumin (ASC-J9), a SARD, is under development for the treatment of acne vulgaris. [2]

In addition, several PROTACs degraders targeting the androgen receptor have been tested in the clinic:

  1. Bavdegalutamide (ARV-110): Developed by Arvinas, this PROTAC is currently in phase 2 clinical trials and has shown encouraging results for patients with metastatic castration-resistant prostate cancer. [3]
  2. Luxdegalutamide (ARV-766) Developed by Arvinas, this second-generation AR PROTAC has advanced to phase II clinical trials. It was designed to overcome some limitations of ARV-110, particularly in targeting the AR L702H mutation. [4] [5]
  3. Gridegalutamide (CC-94676, AR-LDD): Initially developed by Celgene and now under Bristol Myers Squibb (BMS), this AR PROTAC is in phase I clinical trials for patients with metastatic castration-resistant prostate cancer (mCRPC). [4]

See also

References

  1. 1 2 Lai AC, Crews CM (February 2017). "Induced protein degradation: an emerging drug discovery paradigm". Nature Reviews. Drug Discovery. 16 (2): 101–114. doi:10.1038/nrd.2016.211. PMC   5684876 . PMID   27885283.
  2. ↑ "ASCJ 9". AdisInsight. Springer Nature Switzerland AG.
  3. ↑ Jia X, Han X (February 2023). "Targeting androgen receptor degradation with PROTACs from bench to bedside". Biomedicine & Pharmacotherapy. 158 114112. doi: 10.1016/j.biopha.2022.114112 . PMID   36508999.
  4. 1 2 Israel JS, Marcelin LM, Thomas C, Szczyrbová E, Fuessel S, Puhr M, et al. (July 2024). "Emerging frontiers in androgen receptor research for prostate Cancer: insights from the 2nd international androgen receptor Symposium". Journal of Experimental & Clinical Cancer Research. 43 (1): 194. doi: 10.1186/s13046-024-03125-5 . PMC   11253403 . PMID   39014480.
  5. ↑ Chen QH, Munoz E, Ashong D (February 2024). "Insight into Recent Advances in Degrading Androgen Receptor for Castration-Resistant Prostate Cancer". Cancers. 16 (3): 663. doi: 10.3390/cancers16030663 . PMC   10854644 . PMID   38339414.
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