Vosilasarm

Not to be confused with Trestolone.
Vosilasarm
Clinical data
Other namesRAD140; RAD-140; EP0062; Testolone; Testalone
Routes of
administration		By mouth[1][2]
Pharmacokinetic data
Elimination half-life45–60 hours[2][3]
Identifiers
  • 2-Chloro-4-{[(1R,2S)-1-[5-(4-cyanophenyl)-1,3,4-oxadiazol-2-yl]-2-hydroxypropyl]amino}-3-methylbenzonitrile
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC20H16ClN5O2
Molar mass393.83 g·mol−1
3D model (JSmol)
  • ClC1=C(C#N)C=CC(=C1C)N[C@H]([C@H](C)O)C2=NN=C(O2)C3=CC=C(C=C3)C#N
  • InChI=1S/C20H16ClN5O2/c1-11-16(8-7-15(10-23)17(11)21)24-18(12(2)27)20-26-25-19(28-20)14-5-3-13(9-22)4-6-14/h3-8,12,18,24,27H,1-2H3/t12-,18+/m0/s1
  • Key:XMBUPPIEVAFYHO-KPZWWZAWSA-N

Vosilasarm, also known by the development codes RAD140 and EP0062 and by the black-market name Testolone or Testalone, is a selective androgen receptor modulator (SARM) which is under development for the treatment of hormone-sensitive breast cancer.[4][5][6][7] It is specifically under development for the treatment of androgen receptor-positive, estrogen receptor-negative, HER2-negative advanced breast cancer.[4][5][8] Vosilasarm was also previously under development for the treatment of sarcopenia (age-related muscle atrophy), osteoporosis, and weight loss due to cancer cachexia, but development for these indications was discontinued.[4][9] The drug is taken by mouth.[1][2]

Side effects of vosilasarm may include vomiting, dehydration, constipation, decreased appetite, weight loss, changes in sex hormone levels, elevated liver enzymes, and liver toxicity.[2][10][11][12][13][14] Vosilasarm is a nonsteroidal SARM, acting as an agonist of the androgen receptor (AR), the biological target of androgens and anabolic steroids like testosterone and dihydrotestosterone (DHT).[15][7] However, it shows dissociation of effect between tissues in preclinical studies, with agonistic and anabolic effects in muscle, agonistic effects in breast, and partially agonistic or antagonistic effects in the prostate gland and seminal vesicles.[6][7][9][15][16]

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 1/2 clinical 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 Agency list 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]

  1. ^ a b c d Hall E, Vrolijk MF (July 2023). "Androgen Receptor and Cardiovascular Disease: A Potential Risk for the Abuse of Supplements Containing Selective Androgen Receptor Modulators". Nutrients. 15 (15): 3330. doi:10.3390/nu15153330. PMC 10420890. PMID 37571268.
  2. ^ a b c d e LoRusso 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. PMID 34565686. S2CID 237943992.
  3. ^ a b Hamilton E, LoRusso P, Ma C, Vidula N, Bagley RG, Troy S, et al. (2020-02-15). "Abstract P5-11-01 : Phase 1 dose escalation study of a novel selective androgen receptor modulator (SARM), RAD140, in estrogen receptor positive (ER ), human epidermal growth factor receptor 2 negative (HER2-), metastatic breast cancer". Cancer Research. 80 (4 Supplement): P5–11–01. doi:10.1158/1538-7445.sabcs19-p5-11-01. S2CID 216326672.
  4. ^ a b c d e "Vosilasarm - Ellipses Pharma". AdisInsight. Springer Nature Switzerland AG.
  5. ^ a b c "Our Portfolio | Ellipses Pharma". Ellipses Life. Retrieved 11 October 2023.
  6. ^ a b c d e Cite error: The named reference pmid33148520 was invoked but never defined (see the help page).
  7. ^ a b c Zhang X, Sui Z (February 2013). "Deciphering the selective androgen receptor modulators paradigm". Expert Opinion on Drug Discovery. 8 (2): 191–218. doi:10.1517/17460441.2013.741582. PMID 23231475. S2CID 2584722.
  8. ^ 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
  9. ^ a b c Cite error: The named reference pmid24900290 was invoked but never defined (see the help page).
  10. ^ a b Hamilton E, Vidula N, Ma C, LoRusso P, Bagley RG, Yu Z, et al. (2019). "Phase I dose escalation study of a selective androgen receptor modulator RAD140 in estrogen receptor positive (ER+), HER2 negative (HER2-) breast cancer (BC)". Annals of Oncology. 30: v123. doi:10.1093/annonc/mdz242.038.
  11. ^ Cite error: The named reference pmid37218811 was invoked but never defined (see the help page).
  12. ^ Cite error: The named reference FloresChitturi2020 was invoked but never defined (see the help page).
  13. ^ Cite error: The named reference pmid36479151 was invoked but never defined (see the help page).
  14. ^ Cite error: The named reference pmid38059982 was invoked but never defined (see the help page).
  15. ^ a b c d Fonseca 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. PMID 32476495. S2CID 219174372.
  16. ^ Yu Z, He S, Wang D, Patel HK, Miller CP, Brown JL, et al. (December 2017). "Selective Androgen Receptor Modulator RAD140 Inhibits the Growth of Androgen/Estrogen Receptor-Positive Breast Cancer Models with a Distinct Mechanism of Action". Clinical Cancer Research. 23 (24): 7608–7620. doi:10.1158/1078-0432.CCR-17-0670. PMID 28974548.
  17. ^ Cite error: The named reference NCT03088527 was invoked but never defined (see the help page).
  18. ^ Cite error: The named reference LimHamiltonPalmieri2023 was invoked but never defined (see the help page).
  19. ^ "The Prohibited List".
  20. ^ Van Wagoner RM, Eichner A, Bhasin S, Deuster PA, Eichner D (November 2017). "Chemical Composition and Labeling of Substances Marketed as Selective Androgen Receptor Modulators and Sold via the Internet". JAMA. 318 (20): 2004–2010. doi:10.1001/jama.2017.17069. PMC 5820696. PMID 29183075.
  21. ^ Cite error: The named reference pmid35574698 was invoked but never defined (see the help page).