Rentosertib for Health & Longevity - Quick Reference Sheet

Rentosertib for Health & Longevity

Created on 09/11/2026 – Quick Reference based on Evidence Review created using AI4L / Opus 5 Audit

An experimental oral medication that blocks a scar-forming enzyme. One short trial showed lung capacity held on the highest dose while it fell on placebo; blood-protein readings looked younger, but these remain unvalidated laboratory measures. Against this sit dose-related liver injury and diarrhea. Unapproved everywhere, with no legitimate supply route, and almost all evidence produced by the developer. (Full Review)

Protocol

Standard regimen
60 mg once daily
Orally, as a tablet. The dose carried into the 52-week phase 3 study. Competing regimens: 30 mg twice daily, 30 mg once daily.
Food
Fasted
A high-fat meal delays the peak from one hour to three and cuts peak concentration by roughly 37%.
Baseline biomarkers
Gate entry
Transaminases, bilirubin, GGT, alkaline phosphatase, potassium, kidney filtration rate and a cardiac interval all gate entry; failing any means the regimen does not start.
Time to effect
Lung capacity
12 weeks
The lung-capacity difference was measured at 12 weeks; no earlier functional readout has been reported.
Blood proteins
Week 4
Blood-protein changes appear by week 4 and largely plateau there.

Benefits

Contraindications
  • Chronic liver disease (any Child-Pugh class) or fatty liver, including its inflamed form
  • Screening ALT, AST, bilirubin or alkaline phosphatase at or above 1.5× normal; GGT at or above 3×
  • Gilbert's syndrome
  • eGFR below 60 mL/min/1.73 m²
  • QTcF above 450 ms (men) or 470 ms (women)
  • Acute worsening of lung fibrosis within 6 months
  • Current smoking or a positive cotinine test
  • Active, suspected or prior cancer within 5 years
  • HIV infection or significant viral hepatitis
  • Pregnancy, breastfeeding, or no effective contraception to 90 days after the last dose
  • Hypersensitivity to serine/threonine kinase inhibitors
Key Interactions
  • Nintedanib (caution, close monitoring)
  • Pirfenidone (caution)
  • Strong/moderate CYP3A4 inhibitors (contraindicated in trial; ketoconazole, clarithromycin)
  • Strong/moderate CYP3A4 inducers (contraindicated in trial; rifampicin, carbamazepine)
  • Strong/moderate CYP1A2 inhibitors and inducers (contraindicated in trial; fluvoxamine, tobacco smoke)
  • QT-prolonging medications (contraindicated in trial; amiodarone, sotalol, macrolides)
  • Warfarin (contraindicated in trial)
  • Immunosuppressants (contraindicated in trial)
  • Grapefruit, pomelo, Seville orange (contraindicated in trial)
  • St John's wort (caution)
  • Paracetamol, high-dose NSAIDs (caution)
  • Liver-toxic supplements (caution; high-dose green tea extract, kava, ashwagandha)
  • CYP3A4-inhibiting supplements (caution; berberine, high-dose curcumin with piperine)
  • Potassium-lowering supplements (caution; licorice, high-dose caffeine)

Risk & Side Effects

  • Medium: Liver injury and abnormal liver function; diarrhea; low blood potassium; acute worsening of the underlying lung disease
  • Speculative: Increased susceptibility to infection; heart-rhythm effects; consequences of long-term Wnt-pathway suppression

Monitoring

Marker Target Why
ALT 10–25 U/L (men), 8–20 U/L (women) Earliest signal of drug-induced liver stress
AST 10–25 U/L Confirms liver-cell injury alongside ALT
Total bilirubin 0.3–1.0 mg/dL Separates a harmless enzyme rise from true liver injury
GGT 10–25 U/L (men), 8–20 U/L (women) Most sensitive marker of bile-duct and drug-induced liver stress
Alkaline phosphatase 55–90 U/L Distinguishes a bile-duct pattern of injury from a liver-cell pattern
Potassium 4.0–4.5 mmol/L The most frequent adverse event, and low levels lengthen cardiac recovery time
eGFR Above 90 mL/min/1.73 m² Kidney clearance capacity; below 60 disqualifies from every trial
QTcF Below 430 ms (men), below 450 ms (women) Detects additive rhythm risk from co-medication and potassium loss
FVC, percent predicted No established target; track change from baseline, where a 2–6% shift is meaningful The primary efficacy measure in lung fibrosis
DLCO, percent predicted No established target; track change from baseline Gas transfer across the lung membrane, the second pillar of disease staging

Cadence: Liver panel and potassium at weeks 2, 4, 8 and 12, then every 3 months; electrocardiogram at weeks 2, 4, 8, 12, 26, 39 and 52; lung function at weeks 4, 12, 26, 39 and 52.

Qualitative Assessment

  • Cough frequency and disruption of sleep and conversation
  • Breathlessness on a fixed, repeatable task such as one flight of stairs
  • Stool frequency and consistency
  • Energy levels and exercise tolerance across the day
  • Appetite, nausea, right-upper-abdominal discomfort and any yellowing of skin or eyes