Vosilasarm was developed in 2010 and was first described in the literature in 2011.[15][9] It was originally developed by Radius Health and is now under development by Ellipses Pharma.[4][5] The first clinical study of vosilasarm, a small (n=22) phase 1 study in women with metastatic breast cancer, was started in 2017 and completed in 2020, with results published in 2019, 2020, and 2022.[10][3][2][17][15] As of March 2023, vosilasarm is in phase 1/2clinical trials for the treatment of breast cancer.[4][18]
Aside from its development as a potential pharmaceutical drug, vosilasarm is on the World Anti-Doping Agencylist of prohibited substances[19] and is sold for physique- and performance-enhancing purposes by black-market Internet suppliers.[6][1] Vosilasarm is often used in these contexts at doses that have not been evaluated in clinical trials, with unknown effectiveness and safety.[6][1] Many products sold online that are purported to be a specific SARM either contain none or contain other unrelated substances.[6][20]Social media has played an important role in facilitating the widespread non-medical use of SARMs.[21]
Medical uses
Vosilasarm is not approved for any medical use and is not available as a licensed pharmaceutical drug as of 2023.[4]
Vosilasarm has been assessed in clinical trials in women with breast cancer at doses ranging from 50 to 150mg/day, with the maximum safe and tolerated dose being 100mg/day.[10][3][2] The drug sold via black-market Internet suppliers and used non-medically has been reported to be taken at doses of 5 to 30mg/day, with unknown adverse effects and risks.[1][23]
In castrated immature male rats, vosilasarm (at 10mg/kg/day orally, the highest assessed dose) maximally stimulated prostate weight to 67%, seminal vesicle weight to 59%, and levator ani muscle weight to 117% compared to that induced with testosterone propionate 1mg/kg/day.[7][6][9] Moreover, when combined with testosterone propionate, vosilasarm partially antagonized the weight increases of the prostate gland and seminal vesicles, reducing them to 84% and 78% (both from 100%), respectively.[7][9] Conversely however, the combination of testosterone propionate and vosilasarm was additive in terms of levator ani muscle weight stimulation, increasing it to 124%.[7][9] Vosilasarm was found to stimulate muscle at a dose much lower than that required to stimulate the prostate.[7] A dose of 0.3mg/kg/day stimulated levator ani muscle weight to a similar extent relative to the levator ani weight in non-castrated controls.[7][9] Conversely, a 33-fold higher dose of 10mg/kg/day was required to stimulate prostate weight to a similar extent as that in non-castrated controls.[9] Similarly, in gonadally intact immature rats, 0.3mg/kg/day vosilasarm stimulated levator ani muscle weight to a similar extent as testosterone propionate 0.5mg/kg/day, but a dose of 30mg/kg/day (100-fold higher) was required to stimulate the prostate to a similar extent as testosterone propionate 0.5mg/kg/day.[7][6][9] Hence, in rats, vosilasarm is a potent full agonist of the levator ani muscle but a partial agonist and antagonist of the prostate and seminal vesicles, and is strongly selective for stimulating the levator ani muscle over the prostate gland.[7][9] In young male cynomolgus monkeys, vosilasarm, at oral doses of 0.01mg/kg/day, 0.1mg/kg/day, and 1mg/kg/day for 28days, dose-dependently stimulated body weight (+10% at ≥0.1mg/kg/day) and numerically increased lean body mass.[7][6][15][9] The lack of statistical significance was likely due to the small sample sizes per dosing group (n=3 each).[15][9] No data on vosilasarm and lean body mass in humans have been published as of 2022.[2][15]
Vosilasarm was developed by Radius Health in 2010.[15][9] It was first described in in the literature in 2011 in a paper detailing its design, synthesis, and preclinical characterization in vitro and in rats and monkeys.[9] It was stated in this paper that phase 1clinical studies of vosilasarm for treatment of severe weight loss due to cancer cachexia were being prepared.[9][7] However, these studies were never completed or published and development for this indication was discontinued.[4] Subsequently, vosilasarm was repurposed for the treatment of breast cancer.[4]
Society and culture
Names
Vosilasarm is the generic name of the drug and its International Nonproprietary Name (INN).[28] It is also known by its pharmaceutical developmental code names RAD140 (Radius Health) and EP0062 (Ellipses Pharma).[4] Additionally, vosilasarm is known by the black-market name Testolone or Testalone.[15][6][23]
Non-medical use
Vosilasarm and other SARMs are sold by black-market vendors on the Internet.[6][20] Aside from vosilasarm, the other most commonly used SARMs include enobosarm (ostarine; GTx-024, S-22), LGD-4033 (VK5211; "ligandrol"), and andarine (GTx-007; S-4).[21]Social media has played an important role in facilitating the widespread non-medical use of SARMs.[21]
Research
The first-in-human study, a phase 1 trial, was initiated in October 2017 and completed in September 2020 in postmenopausal women with breast cancer.[10][3][2][17][15] The study investigated oral doses of vosilasarm of 50mg/day to 150mg/day, with the maximum tolerated dose found to be 100mg/day.[10][3][2] A phase 1/2 study proposal of vosilasarm for treatment of breast cancer was published in 2023.[18] It will recruit up to 128patients.[18]
^ abcdefghijklLoRusso P, Hamilton E, Ma C, Vidula N, Bagley RG, Troy S, et al. (January 2022). "A First-in-Human Phase 1 Study of a Novel Selective Androgen Receptor Modulator (SARM), RAD140, in ER+/HER2- Metastatic Breast Cancer". Clinical Breast Cancer. 22 (1): 67–77. doi:10.1016/j.clbc.2021.08.003. PMID34565686. S2CID237943992.
^ abcdefghijklmnopMachek SB, Cardaci TD, Wilburn DT, Willoughby DS (December 2020). "Considerations, possible contraindications, and potential mechanisms for deleterious effect in recreational and athletic use of selective androgen receptor modulators (SARMs) in lieu of anabolic androgenic steroids: A narrative review". Steroids. 164: 108753. doi:10.1016/j.steroids.2020.108753. PMID33148520. S2CID225049089.
^Clinical trial number NCT05573126 for "Phase 1/2 Study to Evaluate EP0062 in Patients With Relapsed Locally Advanced or Metastatic Androgen Receptor Positive (AR+)/HER2-/ER+ Breast Cancer" at ClinicalTrials.gov
^ abcdefghijkFonseca GW, Dworatzek E, Ebner N, Von Haehling S (August 2020). "Selective androgen receptor modulators (SARMs) as pharmacological treatment for muscle wasting in ongoing clinical trials". Expert Opinion on Investigational Drugs. 29 (8): 881–891. doi:10.1080/13543784.2020.1777275. PMID32476495. S2CID219174372.
^ abClinical trial number NCT03088527 for "Phase 1, First-in-Human Study of RAD140 in Postmenopausal Women With Breast Cancer" at ClinicalTrials.gov
^ abcLim E, Hamilton E, Palmieri C, Arkenau HT, Brook S, Fisher G, et al. (1 March 2023). "Abstract OT1-02-02: A phase 1/2 study to evaluate the safety and efficacy of EP0062, an oral Selective Androgen Receptor Modulator (SARM), for the treatment of AR+/HER2-/ER+ advanced breast cancer". Cancer Research. 83 (5_Supplement): OT1–02–02-OT1-02-02. doi:10.1158/1538-7445.SABCS22-OT1-02-02. ISSN1538-7445. S2CID257320030.
^Wu C, Kovac JR (October 2016). "Novel Uses for the Anabolic Androgenic Steroids Nandrolone and Oxandrolone in the Management of Male Health". Current Urology Reports. 17 (10): 72. doi:10.1007/s11934-016-0629-8. PMID27535042. S2CID43199715.
^ abMohler ML, Nair VA, Hwang DJ, Rakov IM, Patil R, Miller DD (2005-10-28). "Nonsteroidal tissue selective androgen receptor modulators: a promising class of clinical candidates". Expert Opinion on Therapeutic Patents. 15 (11). Informa Healthcare: 1565–1585. doi:10.1517/13543776.15.11.1565. ISSN1354-3776. S2CID96279138.
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