Rentosertib timeline

Insilico Medicine founded

Alex Zhavoronkov founded Insilico Medicine while at Johns Hopkins University in Baltimore, initially working on ageing biology and machine learning rather than drug development. Source

PandaOmics ranks TNIK as the top anti-fibrosis target

Insilico says its PandaOmics software analysed multi-omics data and text from patents, publications, grants and trials, returned about 20 candidate targets for idiopathic pulmonary fibrosis and placed TNIK first. Source

Chemistry42 designs the molecule that becomes rentosertib

Insilico reports that 79 molecules were synthesised from generative designs and that the 55th was selected, which is where the internal code ISM001-055 comes from. Source

ISM001-055 nominated as a preclinical candidate

The company says the programme reached preclinical candidate stage in about 18 months for roughly US$2.6m, figures that come from Insilico and have not been independently audited. Source

Preclinical candidate announced publicly

Insilico announced the candidate as an industry first for a molecule whose target and structure were both selected using AI, a framing several commentators disputed at the time. Source

Series C raises US$255m

Warburg Pincus led the round, the largest private financing Insilico had raised to that point. Source

Phase 0 microdose study begins in Adelaide

Eight healthy volunteers received a single 100 microgram intravenous dose in Australia under registration ACTRN12621001541897. Source

First participant dosed in Phase 1, New Zealand

The single and multiple ascending dose study NCT05154240 began in Christchurch and eventually enrolled 78 healthy volunteers. Source

Insilico claims target discovery to Phase 1 in under 30 months

The company announced the milestone as evidence that AI had shortened early development, a claim that rests on its own internal timeline. Source

China's regulator clears a Phase 1 application

The Center for Drug Evaluation approved Insilico's first clinical study in China for ISM001-055. Source

Series D opens and Feng Ren becomes co-chief executive

An initial US$60m was announced, later extended to US$95m with backing from Prosperity7, the venture arm of Aramco. Source

First dosing in the China Phase 1 study

Study CTR20221542 began at Zhejiang Xiaoshan Hospital in Hangzhou and enrolled 48 healthy volunteers. Source

Sanofi collaboration announced, up to US$1.2bn

A target discovery and design deal that does not involve rentosertib, with up to US$21.5m payable upfront. Source

Phase 1 topline results reported from New Zealand

Insilico reported no deaths and no serious adverse events, with all treatment-related adverse events described as mild. Source

FDA grants orphan drug designation for IPF

Orphan designation gives commercial incentives for rare disease medicines and is not an assessment of whether a medicine works. Source

Phase 2a trial GENESIS-IPF starts in China

NCT05938920 opened at sites across China to test 30 mg once daily, 30 mg twice daily and 60 mg once daily against placebo for 12 weeks; the Nature Medicine paper gives the start date as 19 July 2023. Source

Financial Times reports the first human trials of an AI-designed drug

Jamie Smyth's piece was the landmark international story on the programme and called the trial a moment of truth for AI drug discovery. Source

Exelixis licenses ISM3091 for US$80m upfront

An oncology programme, not rentosertib, which Insilico has never out-licensed. Source

United States Phase 2a trial begins

NCT05975983 opened at 12 US sites with Toby Maher as lead investigator; it was still listed as recruiting in September 2026 and has reported no results. Source

Nature Biotechnology publishes the discovery-to-clinic paper

Ren and colleagues set out the target selection, generative chemistry and preclinical work behind rentosertib. Source

MIT Technology Review questions the AI discovery claim

Antonio Regalado's piece quoted Recursion's chief executive describing the programme as one of many that have claimed to be first. Source

Last patient visit in the China Phase 2a trial

The registry records study completion on 8 August 2024 after 71 participants were randomised from 128 screened. Source

Headquarters moves to Cambridge, Massachusetts

The company relocated its head office from Hong Kong to 1000 Massachusetts Avenue while keeping its main laboratories in China. Source

Journal of Medicinal Chemistry paper on the molecule

A medicinal chemistry account of how the series was optimised into the compound taken into trials. Source

Phase 2a topline results announced

Insilico's announcement used an analysis that excluded outliers, giving a placebo change of −62.3 mL rather than the −20.3 mL later published in Nature Medicine. Source

BBC News covers AI drug discovery, including rentosertib

Professor Charlotte Deane of Oxford told the BBC there is no agreed definition of what counts as an AI-discovered drug. Source

USAN Council approves the name rentosertib

The stem -sertib marks a serine/threonine kinase inhibitor; the first part of the name derives from co-chief executive Feng Ren. Source

China grants breakthrough therapy designation

The Center for Drug Evaluation designation speeds up regulatory interaction and does not mean the medicine has been shown to work. Source

Nature Medicine publishes the Phase 2a results

The paper reports a forced vital capacity change of +98.4 mL in the 18 people on 60 mg once daily against −20.3 mL on placebo, alongside 16 of 71 participants discontinuing and seven liver-related withdrawals. Source

The Times publishes the only UK national newspaper piece on rentosertib

Tom Whipple's column treated the result as evidence that AI will change drug discovery; no UK national outlet reported the Phase 2a paper as news. Source

Qureight of Cambridge publishes an imaging analysis of the Phase 2a scans

The deep-learning analysis reported no baseline imbalance in disease severity and is the only documented UK commercial involvement in the programme. Source

Chemistry World publishes a sceptical assessment

Anthony King's feature gathered critical views from Derek Lowe, Andreas Bender and Chris Meier on how much AI actually contributed. Source

Phase 2a data presented at the European Respiratory Society congress

Abstract OA1251 was presented in Amsterdam; a congress highlights write-up later misreported a subgroup figure as a whole-cohort result. Source

Full Phase 2a results posted on ClinicalTrials.gov

The registry posting gave arm-by-arm adverse event rates, including serious or severe events in 38.9% of the 60 mg once daily group against 17.6% on placebo. Source

South China Morning Post reports the liver safety findings

One of the few outlets to give the liver-related discontinuations the same prominence as the lung function result. Source

Insilico Medicine lists on the Hong Kong Stock Exchange

The flotation raised HK$2.277bn, about US$293m, with cornerstone investors including Eli Lilly, Tencent and Temasek; shares closed about 45% above the offer price. Source

The Economist uses rentosertib as its main AI drug case study

The piece placed the programme at the centre of a wider argument about whether AI is changing how medicines are found. Source

Shares join Hong Kong Stock Connect and the Hang Seng Composite

The stock was trading about 139% above its offer price at that point. Source

BBC Future covers AI drug discovery in incurable diseases

Laurie Clarke's piece mentioned rentosertib in passing; UK coverage of the programme has been sparse throughout. Source

Eli Lilly deal worth up to about US$2.75bn

US$115m was payable upfront for oral therapeutics programmes; the deal does not cover rentosertib, which Insilico still owns outright. Source

China clears an inhaled formulation for human testing

The nebulised inhalation solution became Insilico's 13th investigational new drug clearance; no trial had started by September 2026. Source

UK clinical trial reforms come into force

The new regulations, made as SI 2025/538, streamline approvals and set rules on trial transparency and recruitment advertising in the UK. Source

MHRA launches an AI sandbox for medicines

Announced by Lord Vallance at London Tech Week, the scheme takes five initial projects; rentosertib is not among them. Source

The UK ILD Registry closes after 13 years

The British Thoracic Society registry had recorded 12,897 people, 9,485 of them with IPF, across 107 hospitals; it is no longer accepting new entries. Source

Phase 3 trial GENESIS-IPF-3 announced

The 320-participant, 52-week, placebo-controlled trial is registered as NCT07687459 and runs at 47 centres in China only. Source

MHRA licenses nerandomilast, the first new UK IPF medicine in over a decade

Boehringer Ingelheim's nerandomilast, sold as Jascayd, was authorised in Great Britain ahead of the European Union. Source

Nature Reviews Drug Discovery review finds limited clinical impact from AI discovery

Bender, Thomas, Scannell and colleagues concluded that evidence of clinically relevant impact is so far disappointingly limited. Source

NICE draft guidance says nerandomilast should not be used on the NHS

The draft in appraisal GID-TA11552 turned on cost-effectiveness against newly available generic nintedanib; two charities objected during consultation. Source

MIT Technology Review examines who is named as inventor

The piece noted that the two key patents, US 11,795,160 and US 11,739,078, name five human inventors and no software. Source

Insilico reports its first profitable half-year

Revenue of US$106.3m for the six months to 30 June 2026 was up 287% year on year, with a net profit of US$35.54m and cash of US$584.8m. Source

Nature Biotechnology publishes the ageing-clock analysis

An exploratory analysis of 42 Phase 2a participants using six proteomic clocks; 21 of 54 comparisons met the paper's significance threshold and the authors concede the clocks cannot separate ageing from a treated lung. Source

IBTimes UK reports the ageing findings

The only UK consumer outlet to cover the ageing analysis; it noted that only 21 of 54 comparisons reached the significance threshold. Source

First patient dosed in the Phase 3 trial

Dosing began at Peking Union Medical College Hospital in Beijing and at Shanghai Pulmonary Hospital the same day; the principal investigator estimated three to four years to approval under favourable conditions. Source

Second NICE committee meeting on nerandomilast expected

The committee reconvenes after consultation on the negative draft guidance. Source

Final NICE guidance on nerandomilast expected

The outcome will show what any new IPF medicine, including rentosertib if it is ever filed in the UK, would have to clear. Source

Estimated completion of the Phase 3 trial

The registry gives an estimated completion date of 30 October 2029 for GENESIS-IPF-3; commentators have suggested a primary readout is unlikely before late 2027 at the earliest. Source