RAD-140 (Testolone)

Structure: Non-steroidal SARM with a pyrazolo-quinoline backbone. High androgen receptor binding affinity and full agonism in muscle tissue. Its chemical structure produces a hepatotoxicity profile closer to a 17-alpha alkylated oral steroid than other SARMs.

Dosage:

• Bodybuilding: 10-20 mg/day for 8-12 weeks
• Phase I breast cancer trial (Radius Health): 50-200 mg/day (trial discontinued due to adverse events)
• Conservative starting dose: 5-10 mg/day

Administration:

• Oral. No injection required.
• Available as raw powder, liquid suspension, or capsule (research-chemical grade; no approved pharmaceutical form).
• Once-daily dosing due to long half-life (~60 hours).

Key Notes:

• Highest hepatotoxicity risk of commonly used SARMs based on published case report severity. Leung et al. (2022) reported a bilirubin of 38.5 mg/dL after 5 weeks of use, requiring hospitalisation. Pattern is cholestatic and can mimic primary biliary cholangiopathy.
• Multiple published DILI case reports with cholestatic pattern, including cases progressing to acute liver failure requiring transplant evaluation.
• HPTA suppression is severe: testosterone, LH, and FSH can be suppressed to near-hypogonadal levels within weeks. Full PCT with a SERM is required.
• HDL suppression is marked and consistent. Full lipid panel recommended at baseline and mid-cycle.
• Does not aromatise. Estradiol typically suppressed. DHT is not produced.
• Liver function tests must be checked at baseline, mid-cycle, and post-cycle. Any elevation of bilirubin or ALP in a cholestatic pattern warrants immediate cessation.
• The long half-life (~60 hours) means blood levels accumulate with daily dosing; effects and side effects may be delayed in onset but prolonged on cessation.
• WADA prohibited under S1. Detection window approximately 21 days in urine.
• All available product is research-chemical grade. No approved human pharmaceutical exists.