Table 1.
Timeline for the development of AR antagonists for prostate cancer.
| Generic name | Other name | Approval date (or clinical stage) | Treatments |
|---|---|---|---|
| Fist-generation | |||
| Flutamide | Eulexin | 27 Jan 1989 | mCRPC |
| Bicalutamide | Casodex | 04 Oct 1995 | mCRPC |
| Nilutamide | Nilandron | 09 Sep 1996 | mCRPC (combined with surgical castration) |
| Second-generation | |||
| Enzalutamide | MDV3100 | 31 Aug 2012 | mCRPC |
| 13 Jul 2018 | nmCRPC | ||
| 16 Dec 2019 | mCSPC | ||
| Apalutamide | ARN-509 | 14 Feb 2018 | nmCRPC |
| 17 Sep 2019 | mCSPC/mCRPC | ||
| Darolutamide | ODM-201 | 30 Jul 2019 | nmCRPC |
| Candidates in clinical trials | |||
| Proxalutamide | GT-0918 | Phase II (recruiting) | mCRPC |
| BMS-641988 | Phase I (closure) | CRPC | |
| TQB3720 | Phase I (recruiting) | mCRPC | |
| SHR3680 | Rezvilutamide | Phase I/IIA (complete) | mCRPC |
| TRC-253 | Phase I/IIA (complete) | mCRPC | |
Information is taken from the websites ClinicalTrials.gov (https://clinicaltrials.gov/ct2/home) and Drugs@FDA: FDA-Approved Drugs (https://www.accessdata.fda.gov/scripts/cder/daf/).