News about rentosertib

Clinical Trial Vanguard reported that the primary readout from the Phase 3 trial is unlikely before late 2027. It also reported that Insilico is funding the trial itself from revenue generated by its partnership deals. The trial registry estimates completion in October 2029.

Insilico announced that the first patient had been dosed in GENESIS-IPF-3 at Peking Union Medical College Hospital, with Shanghai Pulmonary Hospital dosing on the same day. The trial plans to enrol 320 people at 47 centres in China and to run for 52 weeks, with completion estimated for October 2029. The principal investigator, Xu, said approval might take ‘three to four years under favourable conditions’.

IBTimes UK was the only UK consumer outlet to cover the ageing analysis. Its headline says the drug appears to reverse biological age by up to six years, which goes beyond the peak of about three to four years at week 4 reported in the paper. The article does note that only 21 of 54 comparisons reached a Q value below 0.10 and that LTBP2, a fibrosis protein, was the largest contributor.

USA Today covered the ageing-clock analysis under the headline ‘AI drug rentosertib may slow aging. What testing found.’ Alex Zhavoronkov told the paper: ‘There’s no drug that we know of … that can extend life of already optimized individuals.’ No trial has measured whether rentosertib affects lifespan.

Bloomberg’s report, carried by the Japan Times, covered the presentation of the ageing-clock work at a Nature conference at the Sorbonne. The findings come from a secondary analysis of a small Phase 2a trial. That trial’s primary purpose was to assess safety in people with IPF.

Longevity.Technology reported that four of the five ageing-clock teams whose models were used are co-authors on the Nature Biotechnology paper, leaving only the PAC clock independent. It also noted the paper’s own caveat that the clocks cannot separate ageing effects from disease effects. The analysis covers 42 people over 12 weeks.

Insilico announced the proteomic ageing-clock analysis alongside the Nature Biotechnology paper. The analysis covers 42 people from a 71-patient, 12-week trial and measures predicted biological age, not lifespan or health outcomes. Four of the five clock teams whose methods were used are co-authors on the paper.

The authors analysed samples from 42 Phase 2a participants against six proteomic ageing clocks, reporting a peak reduction in predicted biological age of about three to four years at week 4 in the 30 mg twice daily group. The paper states that the clocks ‘cannot deconvolute aging- and disease-specific effects’. Only 21 of 54 comparisons reached a Q value below 0.10, the effect had plateaued by week 12, and the relationship between FVC change and predicted age change was weak (R squared about 0.06). The largest single contributor was LTBP2, a protein associated with fibrosis, and Alex Zhavoronkov, Insilico’s chief executive, is the first author.

Cade Metz reported the ageing-clock analysis under the headline ‘Early Data Indicates an A.I.-Generated Drug Could Slow Aging’. The report is hedged throughout and attributes the claim to the company, using the phrase ‘its maker says’. The underlying analysis is exploratory and covers 42 people over 12 weeks.

The Wall Street Journal ran a sceptical-leaning piece on Feng Ren’s ambitions for rentosertib beyond fibrosis. The article sets out the company’s argument that an antifibrotic drug might also affect ageing biology. No trial has tested rentosertib with an ageing outcome as its endpoint.

NICE published draft guidance (GID-TA11552) not recommending nerandomilast for routine NHS use, on cost-effectiveness grounds. The medicine had received its MHRA licence seven weeks earlier. A second committee meeting is scheduled for 12 November 2026 and final guidance for 20 January 2027. Any future IPF medicine, rentosertib included, would face the same assessment before the NHS could fund it.

Insilico reported first-half 2026 revenue of US$106.3m, up 287%, and a net profit of US$35.54m. It was the company’s first profitable half year, and cash stood at US$584.8m at 30 June 2026. The revenue comes from partnership deals on other programmes, not from selling any medicine.

The article examined who is named as inventor on the rentosertib patents. US patents 11,795,160 and 11,739,078 name five human inventors and no software. Ryan Abbott, a lawyer and academic who has argued for AI inventorship, is quoted.

Insilico announced a second consecutive Prix Galien USA Best Start-Up nomination. The accompanying release describes the rentosertib Phase 3 as global. The trial runs at 47 centres in China and nowhere else.

Derek Lowe reviewed how AI drug discovery is performing against its claims. He has previously written that the TNIK programme is a step up from other announcements in the field, while remaining unconvinced by broader claims about AI-discovered targets. He describes himself as a short-term pessimist and a long-term optimist.

Bender, Thomas, Scannell and colleagues reviewed the clinical record of drug candidates derived using AI. They concluded that ‘evidence of their clinically relevant impact is, so far, disappointingly limited’. It is the most substantial peer-reviewed assessment of the field’s clinical output to date.

Reuters reported a collaboration between Insilico and Bora Pharmaceuticals with more than US$2.5bn in potential value. Rentosertib is not included. Insilico’s announced deal value for 2026 comes to about US$7.3bn, nearly all of it in milestones that may never be paid.

Drug Target Review, a UK trade title, covered the start of the Phase 3 trial. Its report follows the company announcement closely. UK coverage of the programme remains confined to trade and specialist outlets.

The MHRA granted a marketing authorisation to nerandomilast (Jascayd) for idiopathic pulmonary fibrosis and progressive pulmonary fibrosis. It is the first new UK medicine for IPF in more than a decade. A UK licence does not by itself mean the NHS will fund a medicine; that is decided separately by NICE.

Insilico announced the start of GENESIS-IPF-3, a 320-patient, 52-week trial (NCT07687459 and CTR20262475) with annual decline in forced vital capacity as its primary endpoint. The trial runs at 47 centres in China only, although some company materials describe it as global. Feng Ren described the programme as the product of a ‘biology-first, aging-informed AI workflow’, and Alex Zhavoronkov said it was ‘no longer only a speed story’.

The Wall Street Journal reported a collaboration between Insilico and Takeda with about US$60m upfront and roughly US$600m in total potential value. Rentosertib is not part of the agreement. Insilico says it is funding the rentosertib Phase 3 itself from deal revenue.

Fortune reported an agreement between Insilico and SK Biopharmaceuticals with up to US$18m upfront and more than US$2.5bn in potential milestones. The deal does not involve rentosertib. Headline values of this kind depend on milestones that are rarely all achieved.

The MHRA announced an AI sandbox for medicines development, launched by Lord Vallance at London Tech Week. Five projects were selected for the first cohort. Rentosertib is not among them, and Insilico has no UK regulatory footprint of any kind.

Insilico presented poster 8945 on preclinical work with the inhaled formulation at the ATS 2026 conference in Orlando. The data come from animals, not from people. The conference also listed the programme as a Featured Success Story.

Insilico announced that China’s Center for Drug Evaluation had cleared an investigational new drug application for a nebulised inhalation solution of rentosertib. The company says it is its 13th cleared application. The planned study of about 80 subjects had not been entered on any public trial registry.

The new UK clinical trials regulations (SI 2025/538) took effect, introducing a combined MHRA and ethics review. The government says the reforms are intended to make the UK a faster place to run trials. Rentosertib has never had a UK trial site, and Insilico has made no application to the MHRA.

Insilico announced a longevity board chaired by Andrew Adams, formerly of Eli Lilly, with Michael Levitt among its members. Levitt is a Nobel laureate who has sat on Insilico’s scientific advisory board since 2014, so his comments on the company’s work are not independent. The board was announced several months before Insilico published its ageing-clock analysis.

Reuters reported that Eli Lilly had agreed to pay Insilico US$115m upfront, with up to about US$2.75bn in milestones, for work on oral therapeutics. The agreement does not include rentosertib. Lilly was also a cornerstone investor in Insilico’s December 2025 listing.

Insilico reported 2025 revenue of US$56.24m, down 34.5%, and a net loss of US$352.3m. About US$296.7m of that loss was a non-cash charge related to the listing. The company held US$393.3m in cash and said it had submitted an application for an inhaled formulation. The results made no mention of the previously announced US Phase 2b.

Laurie Clarke’s feature on AI in drug discovery mentions rentosertib in passing. It is one of a small number of UK-published pieces to name the drug at all. The article does not examine the Phase 2a safety findings.

Harvard Business School published a teaching case, ‘Insilico’s Rentosertib Dilemma’, written by Michael Lingzhi Li and first taught in October 2025. The case turns on whether Insilico should license the drug out or develop it itself. Insilico has kept rentosertib and is funding the Phase 3 from its own deal revenue.

The Economist ran a survey of AI in drug discovery with rentosertib as its central example. The piece is framed around speed and cost rather than clinical evidence. At the time of publication the drug had been tested in 71 people with IPF for 12 weeks.

Insilico announced an oncology collaboration with Servier, with US$32m upfront and up to US$888m in total potential value. The agreement does not cover rentosertib. Insilico’s announced deals for 2026 total about US$7.3bn on paper, almost all of it contingent milestone payments.

Insilico listed on the Hong Kong stock exchange as 03696.HK, raising HK$2.277bn (about US$293m) at HK$24.05 a share. The retail tranche was oversubscribed 1,427 times and the shares closed 45.5% above the offer price on the first day. Cornerstone investors included Eli Lilly, Tencent and Temasek. It was the largest Hong Kong biotech listing of 2025 and followed three lapsed filings since 2023.

Xinmei Shen’s report was one of the few to give the liver-related adverse events the same prominence as the lung-function result. Seven of the 71 Phase 2a participants stopped the trial because of liver injury or dysfunction. Most coverage of the trial reported only the FVC figures.

The complete results of the China Phase 2a trial were posted to the registry record for NCT05938920. The posted tables give serious or grade 3 and above adverse events in 38.9% of the 60 mg once daily group against 17.6% on placebo. They also record three acute exacerbations (16.7%) in the 60 mg group against one (5.9%) on placebo, all three requiring admission to hospital.

Insilico presented Phase 2a results at the ERS Congress in Amsterdam as abstract OA1251. The abstract uses the analysis with outliers excluded, giving a placebo change of -62.3 mL rather than the published intention-to-treat figure of -20.3 mL. A separate ERS highlights article by Laura Fabbri of Imperial College London misreports the comparison, setting a subgroup result of +188 mL against the whole-cohort placebo value.

Anthony King’s feature quoted Derek Lowe, Andreas Bender and others on what rentosertib does and does not demonstrate. Bender, a cheminformatics researcher who has held posts at Cambridge and Khalifa University, has said of AI drug discovery that ‘much of the in vivo translation is completely missing’. It is the most detailed sceptical treatment of the programme published by a UK outlet.

WIRED examined why companies using AI for drug discovery had produced so few medicines. The piece set Insilico’s TNIK inhibitor against a sector record that includes Exscientia’s abandoned DSP-1181 and BenevolentAI’s failed BEN-2293. No medicine discovered using AI has been approved anywhere.

Qureight, a Cambridge company, reported a deep-learning analysis of CT scans from the China Phase 2a trial. It said there was no imbalance in baseline disease severity between the trial arms and that the Chinese cohort appeared representative of IPF elsewhere. Qureight is the only UK organisation with any documented involvement in the programme, and there is no evidence that it is involved in the Phase 3. The analysis was announced through the company rather than published in a peer-reviewed journal.

Marinka Zitnik of Harvard wrote a News and Views commentary on the Phase 2a trial, saying: ‘This trial marks a turning point.’ Zitnik has no connection to Insilico, and the piece is one of the few independent positive assessments of the work. It is commentary on a 71-patient, 12-week trial rather than evidence of clinical benefit.

Tom Whipple wrote a column using rentosertib as his example of AI-assisted drug discovery. It is the only piece in a UK national newspaper with rentosertib as its subject. It is a comment column rather than a news report, and no UK national outlet covered the Nature Medicine results as news.

Brian Buntz’s report was among the first to give prominence to the liver-related discontinuations in the Phase 2a trial. Seven of the 12 participants who stopped because of side effects did so for liver injury or dysfunction, and four of those seven were also taking nintedanib. Completion was 67% in the 60 mg once daily group against 88% on placebo.

Alex Philippidis reported that Insilico planned a China Phase 3 of more than 500 patients and a US Phase 2b of more than 200, both to start in the fourth quarter of 2025. The article noted that the US Phase 2a had screened 22 people and enrolled eight. The Phase 3 eventually started in July 2026 with 320 patients, and the US Phase 2b was never registered.

Xu and colleagues published the randomised Phase 2a trial of rentosertib in 71 people with IPF in China. The authors report a change in forced vital capacity (FVC), a measure of how much air you can breathe out, of +98.4 mL in the 60 mg once daily group (95% confidence interval 10.9 to 185.9) against -20.3 mL on placebo over 12 weeks. The primary endpoint was safety; every FVC result was a secondary, unpowered analysis, and no p-values for FVC were reported. Sixteen of the 71 participants (22.5%) left the trial, 12 because of side effects, and 7 of those discontinuations were for liver injury or dysfunction.

Insilico said in June that its Series E round had closed at US$123m, valuing the company at about US$1bn. The company had by then raised more than US$500m in venture funding since 2017.

Insilico presented its China Phase 2a findings at the ATS 2025 international conference. Conference abstracts are not peer reviewed in the way journal papers are. The full paper appeared in Nature Medicine two weeks later.

China’s Center for Drug Evaluation granted breakthrough therapy designation to rentosertib for IPF in May. The designation allows closer contact with the regulator and a faster review in China. It is not an approval, and it has no effect in the UK.

Insilico announced a Series E round of US$110m led by Value Partners. The company said the money would support late-stage work on its TNIK inhibitor. The round closed later in the year at US$123m.

The United States Adopted Names Council assigned the name rentosertib to ISM001-055. Insilico said its co-chief executive Feng Ren proposed the name. The drug had previously appeared in trial registries as INS018_055.

Fierce Biotech reported Insilico’s published benchmarks for how long each of its 22 drug candidates took to reach nomination. The company uses these figures to argue that its software shortens discovery. The comparisons are Insilico’s own and have not been independently verified.

Zoe Corbyn reported on AI methods in drug discovery, including Insilico’s TNIK inhibitor. Charlotte Deane, professor of structural bioinformatics at Oxford, told the BBC there is ‘no definition yet of what exactly counts as an AI discovered drug’. Alex Zhavoronkov said: ‘We can’t say we have the first AI discovered and designed molecule approved. But we may be the furthest along the path.’

Insilico announced topline results from its 71-patient China Phase 2a trial. The release reported a change in forced vital capacity (FVC), a measure of how much air you can breathe out, of +98.4 mL in the 60 mg once daily group against -62.3 mL on placebo. That placebo figure comes from an analysis with outliers excluded; the published intention-to-treat figure is -20.3 mL, and it has not been verified that the exclusion was specified in advance. The trial’s primary endpoint was safety: 12 of the 71 participants stopped because of side effects, 7 of them because of liver injury or liver dysfunction.

GEN reported in November that Insilico intended to take its TNIK inhibitor into a pivotal trial. The company was then describing both a US Phase 2b and a larger Phase 3 in China. The US Phase 2b was never registered.

A paper setting out the medicinal chemistry of ISM001-055 appeared in the Journal of Medicinal Chemistry in October. It describes the bis-imidazolecarboxamide series from which the molecule was selected. No independent analysis of the molecule’s structural novelty has been published.

Endpoints News reported that Insilico’s Hong Kong listing plans had lapsed for a second year running. The company made three filings between 2023 and 2025 before completing its listing in December 2025.

The Boston Globe reported that Insilico had moved its headquarters to 1000 Massachusetts Avenue in Cambridge. The company was founded in Baltimore in 2014 and was later based in Hong Kong. Its listed parent is a Cayman Islands company quoted in Hong Kong.

Insilico issued preliminary results from its China Phase 2a trial ahead of the full topline. The release quoted Toby Maher, a professor at Imperial College London’s National Heart and Lung Institute who is also lead investigator on Insilico’s US Phase 2a trial. His comments appear in the company’s own press release and are not independent commentary.

GEN reported that Insilico had moved its headquarters to Cambridge, Massachusetts and had finished enrolling its China Phase 2a trial. The company had previously been based in Hong Kong and, before that, Baltimore. Its clinical operations remained in China.

A review of TNIK as a drug target appeared in Trends in Pharmacological Sciences in June. TNIK is a kinase involved in Wnt signalling and in fibrosis. The review was published while Insilico’s China Phase 2a trial was still running.

Nature Aging published a research highlight on Insilico’s use of ageing biology to select TNIK as a target. The piece is a commentary rather than new clinical data. Insilico’s later claims about ageing build on this line of work.

Antonio Regalado reported on Insilico’s claim to have reached a milestone with what the company called a factory of drugs. Chris Gibson, chief executive of the rival firm Recursion, told the magazine the programme was ‘one of many programs that have claimed to be first’. The article also covers Alex Zhavoronkov’s comparison of Insilico with Tesla.

Holly Chik reported on Insilico’s TNIK inhibitor and the company’s Hong Kong base. The piece followed the Nature Biotechnology paper describing the discovery process. All clinical work on the drug has been carried out in China, New Zealand and Australia.

C&EN reported on the Nature Biotechnology paper and on how much credit the software deserves. Timothy Cernak of the University of Michigan told the magazine: ‘I think Insilico’s been involved in hyping that, but I think they built something really robust here.’ The article sets out both the claim and the reservations about it.

Ren and colleagues published an account of how Insilico’s software identified TNIK as a target and generated the molecule that became rentosertib. The authors are Insilico employees describing the company’s own platform. The paper covers the preclinical and early clinical work and reports no efficacy result in people with IPF.

The registry record for NCT05975983 gives 8 February 2024 as the start date of a parallel Phase 2a trial in the United States, with an estimated 40 participants at 12 sites and Toby Maher as lead investigator. The listed estimated completion date of 28 February 2026 has since passed with no update. No results have been reported, and the trial record still shows it as recruiting.

Exelixis licensed ISM3091, a USP1 inhibitor, from Insilico for US$80m upfront. The compound is an oncology programme and is unrelated to rentosertib. Insilico has never out-licensed rentosertib and continues to fund it itself.

Insilico announced a preclinical candidate for an inhaled form of its TNIK inhibitor. The company said preclinical work showed high exposure in the lung and low exposure elsewhere in the body. There were no human data for the inhaled form at the time.

Hayden Field reported Insilico’s claim to have produced the first drug with both target and molecule generated by software. The piece noted that no such medicine had been approved anywhere. That remains the case.

Insilico filed its first listing application with the Hong Kong stock exchange. Three separate filings lapsed between 2023 and 2025. The company eventually listed in December 2025.

Insilico announced that the first patients had been dosed in GENESIS-IPF, a Phase 2a trial in China (NCT05938920). The trial compared 30 mg once daily, 30 mg twice daily and 60 mg once daily against placebo over 12 weeks. Its primary endpoint was safety, not lung function.

Jamie Smyth reported that Insilico had begun human trials of a drug designed using artificial intelligence, calling it a ‘moment of truth’ for the field. The article set out the company’s claim that both the target and the molecule came from software. The Financial Times is one of the few UK titles to have covered the programme at all.

The US Food and Drug Administration granted orphan drug designation to ISM001-055 for idiopathic pulmonary fibrosis. Orphan designation provides commercial incentives for rare disease medicines. It is not an assessment of whether a medicine works, and it is not a licence.

Insilico announced a new research centre in Abu Dhabi. The company has offices in Hong Kong, mainland China, the United States, Canada and Taipei. It has never had a UK office, and no Insilico entity has ever been registered at Companies House.

Insilico announced topline results from its New Zealand Phase 1 study. The company reported no deaths and no serious adverse events, and said all treatment-related adverse events were mild. The study enrolled healthy volunteers only, so it says nothing about effects in people with IPF.

Insilico announced a collaboration with Sanofi covering up to six targets, with up to US$21.5m upfront and up to US$1.2bn in total potential payments. The deal does not involve rentosertib, which Insilico owns outright. Almost all of the headline value is milestone payments that may never be earned.

Insilico said it had extended its Series D round to US$95m, with new money from Prosperity7 Ventures, a fund backed by Saudi Aramco. The company said the round would support its clinical pipeline.

Insilico announced first dosing in a Phase 1 study of ISM001-055 at Zhejiang Xiaoshan Hospital in Hangzhou (CTR20221542). The company says the study enrolled about 48 healthy volunteers. That figure comes from company releases rather than a published paper.

Insilico announced a US$60m Series D round and the appointment of Feng Ren as co-chief executive and chief scientific officer. Ren holds a Harvard PhD and had spent 11 years at GSK. The company credits him with leading the TNIK programme.

China’s Center for Drug Evaluation cleared Insilico’s investigational new drug application for a Phase 1 study of ISM001-055 in May. It was the company’s first clinical study in China. The date comes from company materials rather than a public regulatory notice.

Insilico announced that its Phase 0 microdose study in eight healthy volunteers was complete and that a Phase 1 study had begun in Christchurch, New Zealand (NCT05154240). The first participant was dosed on 21 February 2022. Insilico said the programme had gone from target discovery to Phase 1 in under 30 months.

The chemist and blogger Derek Lowe wrote that ISM001-055 was ‘a believable target with believable chemical matter’ and ‘a step up from much of the other AI found a drug! announcements, including some previous hype from Insilico Medicine itself’. He added that Insilico would now be ‘taking their shots the same way as the rest of us’. Lowe describes himself as a short-term pessimist and a long-term optimist about AI in drug discovery.

Insilico reported the start of a Phase 0 microdose study of ISM001-055 in Adelaide, Australia. Eight healthy volunteers received a single 100 microgram intravenous dose. The study was not registered on ClinicalTrials.gov, and detailed numbers appear only in later supplementary material.

Insilico Medicine announced a Series C round of US$255m led by Warburg Pincus. The company said the money would fund its pipeline, including the TNIK inhibitor for IPF. Endpoints News asked in its coverage whether Insilico’s stated development timelines were feasible.

Sam Lemonick reported the preclinical candidate and asked what ‘discovered by AI’ actually means. The article quoted the pharmaceutical analyst Bernard Munos, who questioned how much of the work the software had done. It was the first sceptical coverage of the programme.

Insilico Medicine announced that ISM001-055, later named rentosertib, had been nominated as a preclinical candidate for idiopathic pulmonary fibrosis (IPF). Insilico described this as an industry first because both the target, TNIK, and the molecule came from its own software. The company says the programme took about 18 months and US$2.6m, and that fewer than 80 molecules were synthesised. Insilico’s account of the cost and timeline has not been independently audited.

Conor Hale reported Insilico Medicine’s claim that it had taken both a fibrosis target and a matching molecule from its own software. Insilico said the work took about 18 months. The company had not at that stage published the underlying data.

The Guardian reported on the use of generative software to design new molecules, describing the search space as a ‘molecular casino’. The piece ran four days before Insilico Medicine named its TNIK inhibitor as a preclinical candidate. At that point no molecule designed this way had entered human trials.