Small-molecule inhibitors
A target and a way of hitting it: ATP-competitive, allosteric or covalent kinase inhibitors, PARP trapping, hormone receptor blockade. The grid asks which targets have been hit with which mechanism class. The grid below is target against mechanism class: 114 by 17 from 287 medicines, 93 combinations approved, 31 in development, 5 tried and stopped, 1,811 untried in this corpus.
Every tried combination
Stopped, and why
15 medicines recorded as stopped; 57 recorded reasons, including stopped studies of medicines still in development- ADU-S100 (MIW815)Tried and stopped
ADU-S100 was the first STING agonist in the clinic. Injected directly into tumours, it produced almost no responses, alone or with checkpoint blockade.
- AminoglutethimideTried and stopped
Aminoglutethimide produced a medical adrenalectomy for advanced breast and prostate cancer in the 1970s and 1980s, the ancestor of today's aromatase inhibitors, and was withdrawn once selective drugs arrived.
- CopanlisibTried and stopped
Copanlisib is an intravenous PI3K inhibitor for relapsed follicular lymphoma, approved in 2017 and withdrawn in 2023 when its confirmatory trial failed.
- CopanlisibTried and stopped
Aliqopa accelerated approval Sep 2017; withdrawn by Bayer Nov 2023 after CHRONOS-4
FDA (US): withdrawn 2023 · regulator row
- CopanlisibTried and stopped
Marketing authorisation application withdrawn before a CHMP opinion
EMA / European Commission (EU): withdrawn · regulator row
- EprenetapoptTried and stopped
Eprenetapopt (APR-246) was a drug meant to refold mutant p53, the most common broken protein in cancer. Its phase 3 in blood cancer failed in 2020.
- FormestaneTried and stopped
Formestane, launched in Europe in 1993, was the first selective aromatase inhibitor for advanced breast cancer, given by injection every two weeks; oral exemestane and the non-steroidal inhibitors made it redundant within a few years.
- InfigratinibTried and stopped
Infigratinib is an FGFR inhibitor pill given accelerated approval in the United States in 2021 for bile duct cancer with an FGFR2 fusion, then withdrawn in 2024 when its confirmatory trial could not enrol; it is now being developed for achondroplasia instead.
- IniparibTried and stopped
Billed as the first PARP inhibitor for triple-negative breast cancer, it failed its phase 3 in 2011. It turned out not to inhibit PARP at all.
- MasofanitenTried and stopped
A drug designed to block the part of the androgen receptor that resistant variants keep; its phase 2 was stopped for futility and development ended.
- MobocertinibTried and stopped
Mobocertinib was the first oral drug for EGFR exon 20 insertion lung cancer, approved in 2021 and withdrawn in 2023-24 after its confirmatory trial failed.
- MobocertinibTried and stopped
Exkivity accelerated approval Sep 2021; withdrawn by Takeda Oct 2023 after EXCLAIM-2
FDA (US): withdrawn 2023 · regulator row
- MobocertinibTried and stopped
Marketing authorisation application withdrawn before a CHMP opinion
EMA / European Commission (EU): withdrawn · regulator row
- OlmutinibTried and stopped
Olmutinib was a Korean-developed EGFR pill approved in South Korea in 2016 for lung cancers that had developed the T790M resistance mutation, the same niche as osimertinib; severe skin reactions and osimertinib's success ended its development.
- PanobinostatTried and stopped
An HDAC inhibitor for relapsed myeloma approved in 2015 and withdrawn in 2021 after its confirmatory trial was never completed.
- PanobinostatTried and stopped
Farydak accelerated approval Feb 2015; US approval withdrawn 2022 at Secura Bio's request
FDA (US): withdrawn 2022 · regulator row
- PoziotinibTried and stopped
Poziotinib was a tablet designed to fit the awkward shape of HER2 and EGFR exon 20 mutations in lung cancer. It shrank tumours in some patients but caused severe rash and diarrhoea, and the FDA declined to approve it in 2022.
- ResminostatTried and stopped
CHMP negative opinion 22 May 2025 on Kinselby (4SC) for advanced mycosis fungoides and Sézary syndrome
EMA / European Commission (EU): rejected 2025 · regulator row
- ResminostatTried and stopped
CHMP negative opinion on Kinselby (resminostat) for advanced mycosis fungoides and Sézary syndrome
- TazemetostatTried and stopped
Tazemetostat was the first EZH2 inhibitor, approved for epithelioid sarcoma and follicular lymphoma in 2020 and withdrawn worldwide in 2026 after secondary blood cancers.
- TazemetostatTried and stopped
Withdrawn over secondary haematologic malignancies
- TazemetostatTried and stopped
FDA and Ipsen alignelment: Due to unfeasibility and the resulting inability to meet the required enrolment targets. No safety concerns.
Tazemetostat with doxorubicin as front-line therapy for advanced epithelioid sarcoma (EZH-301 run-in): phase 1, terminated or withdrawn · trial record
- UmbralisibTried and stopped
A PI3K inhibitor for marginal zone and follicular lymphoma approved in 2021 and withdrawn in 2022 after the UNITY-CLL trial suggested more deaths.
- GiredestrantIn development
PFS 33.1 vs 28.2 months, not significant.
persevERA: phase 3, negative · trial record
- AnlotinibApproved
CHMP negative opinion 23 Jul 2026 on Qezzaqar (catequentinib; applicant CATS Consultants) for synovial sarcoma and leiomyosarcoma
EMA / European Commission (EU): rejected 2026 · regulator row
- AvapritinibApproved
PFS HR 1.25 (negative).
VOYAGER: phase 3, negative · trial record
- BelzutifanApproved
Primary endpoint not met (ASCO GU 2026).
LITESPARK-012: phase 3, negative · trial record
- CabozantinibApproved
PFS HR 1.03; OS HR 0.94, negative.
CONTACT-03: phase 3, negative · trial record
- DuvelisibApproved
Authorised May 2021; marketing authorisation withdrawn at Secura Bio's request 16 Feb 2026 (commercial reasons)
EMA / European Commission (EU): withdrawn 2026 · regulator row
- EnasidenibApproved
MAA withdrawn 2021
EMA / European Commission (EU): withdrawn 2021 · regulator row
- EnasidenibApproved
Marketing application withdrawn after EMA objections on efficacy
- ErlotinibApproved
Median overall survival 15.2 months with chemoradiotherapy against 16.5 months with chemotherapy alone (hazard ratio 1.03, p 0.83); local progression 32 against 46 percent; erlotinib added nothing (13.6 against 11.9 months, hazard ratio 1.19).
LAP07: phase 3, negative · trial record
- IbrutinibApproved
MCL and MZL indications voluntarily withdrawn after confirmatory trials missed
Alive at 18 months: 60 percent with neoadjuvant FOLFIRINOX against 73 percent with upfront surgery (p 0.032); median overall survival 25.1 against 38.5 months (hazard ratio 1.52, p 0.050).
NORPACT-1: phase 2, negative · trial record
- LenvatinibApproved
OS HR 0.84, not significant.
LEAP-002: phase 3, negative · trial record
- LenvatinibApproved
Primary endpoint not met (ASCO GU 2026).
LITESPARK-012: phase 3, negative · trial record
- NintedanibApproved
PFS HR 1.01, negative.
LUME-Meso: phase 2/3, negative · trial record
- Omacetaxine mepesuccinateApproved
Tekinex for chronic myeloid leukaemia after imatinib failure, including T315I: marketing authorisation application withdrawn by ChemGenex 11 Jan 2011 at day 120; the CHMP's provisional view was that benefits did not outweigh risks
EMA / European Commission (EU): withdrawn · regulator row
- PalbociclibApproved
PALLAS iDFS HR 0.96; PENELOPE-B iDFS HR 0.93; both null.
PALLAS & PENELOPE-B: phase 3, negative · trial record
- PalbociclibApproved
One year of palbociclib added to endocrine therapy did not improve invasive disease-free survival.
PENELOPE-B: phase 3, negative · trial record
- PalbociclibApproved
PFS 33.1 vs 28.2 months, not significant.
persevERA: phase 3, negative · trial record
- PazopanibApproved
Primary endpoint Progression-free survival
Aldoxorubicin versus investigator's choice in relapsed or refractory soft tissue sarcoma: phase 3, negative · trial record
- PazopanibApproved
Adding TRC105 to pazopanib did not improve progression-free survival; stopped for futility.
TAPPAS: phase 3, negative · trial record
- PemigatinibApproved
The study was terminated due to lack of enrollment resulting from a change in the standard of care for the first-line treatment of patients with cholangiocarcinoma. There were no safety concerns that contributed to this decision.
FIGHT-302: phase 3, terminated or withdrawn · trial record
- PexidartinibApproved
Daiichi Sankyo withdrew the Turalio MAA (Jul 2020) after the CHMP signalled a negative opinion
EMA / European Commission (EU): withdrawn 2020 · regulator row
- PonatinibApproved
Temporary marketing suspension for arterial occlusion; returned with narrowed label December 2013
- PralsetinibApproved
Authorised Nov 2021; marketing authorisation withdrawn at Blueprint's request 24 Oct 2024
EMA / European Commission (EU): withdrawn 2024 · regulator row
- QuizartinibApproved
Complete response letter for relapsed/refractory indication (QuANTUM-R)
- RomidepsinApproved
MAA withdrawn by Celgene before a CHMP opinion
EMA / European Commission (EU): withdrawn · regulator row
- RucaparibApproved
Clovis Oncology bankruptcy; asset sold to pharma&
- RuxolitinibApproved
Complete response within 1 year 46.6% (ruxolitinib) vs 44.2% (best available therapy), not significant; no difference in clots, bleeding or transformation at 2 years.
MAJIC-ET: phase 2, negative · trial record
- SelinexorApproved
Primary PFS endpoint not met; mPFS 12.75 vs 7.43 months (mITT) not significant.
XPORT-EC-042 / ENGOT-EN20 / GOG-3083: phase 3, negative · trial record
- SorafenibApproved
OS not improved; fewer adverse events.
SARAH and SIRveNIB: phase 3, negative · trial record
- SotorasibApproved
FDA declines full approval based on CodeBreaK 200; postmarketing dose study required
- TivozanibApproved
PFS HR 1.10; no benefit from nivolumab rechallenge.
TiNivo-2: phase 3, negative · trial record
- VenetoclaxApproved
Venetoclax added to azacitidine did not significantly improve overall survival in untreated higher-risk myelodysplastic syndromes.
VERONA: phase 3, negative · trial record
- VorinostatApproved
Vorinostat MSD for advanced cutaneous T-cell lymphoma after two systemic therapies: marketing authorisation application withdrawn by MSD 13 Feb 2009 at day 206; the CHMP found benefit not sufficiently demonstrated
EMA / European Commission (EU): withdrawn · regulator row
Not placed
84 of 371 medicines in this format (23%)These medicines belong to the format but their target is on no record the engine reads: the targets field is empty, the target lists no such drug, the trials linked to it name no target of its own, and the modality, mechanism and summary text name none the corpus knows. They are listed here rather than placed by guesswork; adding the target to the record puts them in the grid on the next build.
How this grid is read from the records
Each medicine's parts come from its own record: the targets field first, else the target records that list the medicine, else a sibling conjugate that shares its antibody name, else the trials linked to it, else the target names the corpus knows found in its modality, mechanism or summary text. The second part is read from the medicine's technology links first and from its modality and mechanism text second; a part no record names is shown as not recorded. Every part carries the fields it was read from and a confidence in the JSON file.
What the states mean, and do not
Approved: a medicine in the cell has an approval row or a regulator's approved entry and is not recorded as withdrawn. In development: a recruiting, active or planned trial, a development-phase record status, or active studies in the ClinicalTrials.gov index, and no approval. Tried and stopped: every medicine in the cell is withdrawn, negative or historic, or its only trial evidence is a terminated, withdrawn or negative study, or its approval was withdrawn. Untried: no medicine in this corpus combines the two parts.
A cell is coloured by its strongest medicine; the table shows each medicine with its own state. The reasons quoted under Stopped, and why are the records' words, including the registry's whyStopped text where the sponsor wrote one, and include stopped studies of medicines that are still in development elsewhere. Nothing here is medical advice.