Rentosertib by Insilico Medicine: status and timeline

Rentosertib

Rentosertib is a TNIK inhibitor discovered via AI. It halts lung fibrosis in idiopathic pulmonary fibrosis by blocking TNIK activation. Phase IIa showed dose-dependent lung function preservation.

PilotStage 3 of 5

Phase 3 GENESIS-IPF-3: 320 patients, 52-week placebo trial in China; first dosed Sept 2026.

Updated 9 Sep 2026Checked 10 Oct0 updates this week

Milestones

Next · Phase III GENESIS-IPF-3 first patient dosed

AI target discovery completed2023Complete.
Compound optimization and synthesis2024Complete.
Phase IIa GENESIS-IPF-1 dosing begins2024Complete.
Phase IIa shows dose-dependent efficacy; Nature Medicine publication2025Complete.
Phase III GENESIS-IPF-3 first patient dosedTarget 9 Sep 2026Current milestone.
Phase III trial completion (52 weeks)Target Q3 2027Not yet reached.

Most important updates

Upcoming

9 Sep 2026Phase III GENESIS-IPF-3 first patient dosed (next)
Q3 2027Phase III trial completion (52 weeks)
Q3 2027Phase III primary endpoint read

Current obstacles

Validating AI-discovered drugs clinicallyFirst Phase 3 for an AI drug; success proves the model, failure may slow adoption.
IPF patient heterogeneityPatients progress at different rates. Trial must capture variability to prove efficacy.

Physics limits

Fibrosis is partially irreversibleCollagen scars do not regrow. Blocking TNIK slows new fibrosis but cannot restore lost lung.
Off-target TNIK inhibitionTNIK in other tissues may cause side effects; determining the tolerable dose is critical.

How it works

3 parts

TNIK blocking

Halting the fibrosis cascade

TNIK activation drives collagen deposition in lung fibrosis. Blocking it halts scarring and preserves lung function.

AI-designed

Generative AI found the target

AI identified TNIK as a fibrosis driver and designed the molecule, not by screening but by generation.

Longevity signal

Aging clock improvements

Secondary analysis showed ~3-4 years younger on six aging clocks, hinting at longevity benefits beyond IPF.

Spec sheet

Spec	Rentosertib
Target protein	TNIK (Serine/threonine-protein kinase tousled-like 1)^R (reported)
Primary indication	Idiopathic pulmonary fibrosis (IPF)^R (reported)
Phase 3 trial enrollment	320 participants across 47 centers in China^R (reported)
Phase 3 study duration	52 weeks^R (reported)
Phase IIa FVC decline rate	Dose-dependent reduction^R (reported)

^R reported by the company

Papers & demos

3 items

2026paper
Biological age reduction with Rentosertib (opens nature.com)Novel analysis showing aging-clock improvements, suggesting potential longevity benefits beyond IPF indication.
2025paper
Phase IIa efficacy of Rentosertib in IPF (opens nature.com)Shows dose-dependent efficacy of AI-discovered drug in human clinical trials.
2024paper
AI-driven target discovery for drug discovery (opens nature.com)Demonstrates the scientific foundation for discovering disease targets using generative AI.

Update log

2 updates

Wed 9 Sep

Major: First patient dosed in GENESIS-IPF-3 Phase III trial of AI-discovered drug RentosertibPressTest

Jul 2026

Major: Insilico launches Phase III trial for Rentosertib, first AI-discovered drug in Phase 3PressTest

About Insilico Medicine

The team behind Rentosertib

Insilico Medicine

AI drug discovery, generative AI, molecular design, clinical trials

Insilico uses generative AI to discover drug candidates. The Pharma.ai platform covers target discovery, chemistry, clinical design, and research tools. Founded in 2014, it went public in late 2025.

Insilico went public on Hong Kong Stock Exchange in late 2025, raising approximately $293 million.
In March 2026, Insilico signed a $2.75B AI drug discovery agreement with Eli Lilly.
$106M revenue in H1 2026 (287% YoY growth), with $51M adjusted net profit.

insilico.com (opens insilico.com)Company profile →

Founded: 201412 yrs
Headquarters: Canada
Status: Public
Listed: 3696 (opens google.com)HKEX
Valuation: $1.9Bmarket capDec 2025
Staff: ~350Sep 2026
Raised: $360M4 rounds
Last round: IPO (Hong Kong Stock Exchange) · $293MDec 2025
Works in: BiotechAI drug discoveryLongevity
Coverage: 1 program · 5 updateslatest 9 Sep 2026checked 10 Oct
Partners: Eli Lilly (opens insilico.com)Exelixis (opens exelixis.com)Menarini (opens menarini.com)TaiGen (opens taigenbiotech.com)
People: Alex Zhavoronkov (opens en.wikipedia.org)Founder and CEO

Spec

Rentosertib

Target protein

TNIK (Serine/threonine-protein kinase tousled-like 1)^R (reported)

Primary indication

Idiopathic pulmonary fibrosis (IPF)^R (reported)

Phase 3 trial enrollment

320 participants across 47 centers in China^R (reported)

Phase 3 study duration

52 weeks^R (reported)

Phase IIa FVC decline rate

Dose-dependent reduction^R (reported)