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| Other names | GTx-007; S-4; Acetamidoxolutamide; Androxolutamide; Acetam-doxolutamide |
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| ECHA InfoCard | 100.230.653 |
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| Formula | C19H18F3N3O6 |
| Molar mass | 441.363 g·mol−1 |
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Andarine (developmental code namesGTx-007,S-4) is aselective androgen receptor modulator (SARM) which was developed byGTX, Inc for the treatment of conditions such asmuscle wasting,osteoporosis, andbenign prostatic hyperplasia (BPH),[1] using thenonsteroidal antiandrogenbicalutamide as a lead compound.[2] Development of andarine for all indications has been discontinued, in favor of the structurally related and improved compoundenobosarm (ostarine; GTx-024; S-22).[3]
Andarine is an orally activepartial agonist of theandrogen receptor (AR). In intact male rats, 0.5 mg andarine daily was shown to reduce prostate weight to 79.4%, and non-significantly increasedlevator ani muscle weight. In castrated male rats, this dose restored only 32.5% prostate weight, but 101% levator ani muscle weight[4] This suggests that andarine is able to competitively block binding ofdihydrotestosterone to its receptor targets in the prostate gland, but its partial agonist actions at the androgen receptor prevent the side effects associated with the antiandrogens traditionally used for treatment of BPH.[5]
Andarine was first described in the literature by 2002.[6][7][8] It completedphase 1clinical trials forcachexia in 2003.[9][10] Three phase 1 trials (1a, 1b, 1c) were completed with the drug involving 86 healthy male and female volunteers.[10]Phase 2 trials were planned for 2004.[10] However, development of andarine was discontinued, reportedly due to findings ofvisual disturbances in clinical studies.[3][11] Andarine is thought to have been the first SARM to enter human clinical trials.[12]
The peripheral and selective anabolic preclinical pharmacodynamic profile of 8 seemed highly promising and 3602 Journal of Medicinal Chemistry, 2009, Vol. 52, No. 12 Award Address stimulated us to pursue landmark clinical trials of the SARMs, andarine 8 and Ostarine.75 Although phase I studies with 8 were successful with no deficiencies noted (March 17, 2004, press release), Ostarine was selected for advanced clinical development based on corporate strategy. Readers are cautioned to note that the name Ostarine is often mistakenly linked to the chemical structure of 8, which is also known as andarine. The chemical structure of Ostarine has not been publicly disclosed. The authors are unable to provide additional information.
Clinical Trials. We have completed three Phase I clinical trials of Andarine in a total of 86 healthy male and female volunteers. We tested Andarine for safety and tolerance in single and multiple doses. Results from our Phase I trials support once-a-day oral dosing, and no serious adverse events were observed at any single or multiple dose tested. We observed early indications in the multiple-dose Phase I clinical trial in men that Andarine promoted growth activity, as measured by levels of a growth factor in the blood known as IGF-1, without affecting the sebaceous glands. We believe that these observations support the potential ability of Andarine to selectively modulate androgen receptors in a tissue-specific manner.
S-4 [Andarine, S3-(4-acetylamino-phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamide] a member of the aryl propionamide class of SARMs was evaluated in a phase I clinical trial, but the study had to be stopped due to adverse side-effects involving visual disturbances.[3]
We believe Andarine represents the first SARM to enter human clinical trials.