Small-molecule kinase inhibitors

Acalabrutinib is a cleaner BTK blocker with fewer heart and bleeding problems than ibrutinib. In February 2026 it became half of the first all-oral, fixed-duration CLL regimen.

Afatinib (Gilotrif) is a second-generation pill that binds EGFR, HER2 and HER4 irreversibly, approved in 2013 for EGFR-mutant lung cancer. Its lasting value is activity against the uncommon EGFR mutations G719X, L861Q and S768I, approved in 2018, because osimertinib has displaced it for common mutations and its wild-type EGFR binding causes more rash and diarrhoea.

Alectinib is a well-tolerated ALK pill, standard first line for years and, since 2024, the first targeted therapy given after surgery for ALK-positive lung cancer.

Alpelisib was the first PI3K drug for PIK3CA-mutant breast cancer (2019). It is effective, but high blood sugar and rash limited its use, and newer drugs are displacing it.

Anlotinib is one of the most used cancer pills in China, first approved for lung cancer after other treatments have failed and then for several rarer tumours.

Asciminib is a BCR::ABL1 blocker that binds a different pocket from every other TKI, approved for all newly diagnosed chronic myeloid leukaemia in 2024 and now being tested in Ph-positive ALL.

Aumolertinib is Hansoh's third-generation lung cancer pill, the first China-developed drug of its class, approved for first-line EGFR-mutant lung cancer on the AENEAS trial.

Avapritinib is the first drug for GIST driven by the PDGFRA D842V mutation, which resists every other kinase inhibitor; it is also approved for systemic mastocytosis.

Avutometinib plus defactinib is the first treatment approved specifically for low-grade serous ovarian cancer, a slow-growing type driven by the RAS pathway.

Axitinib is a selective VEGF-receptor pill, now given mainly with pembrolizumab or avelumab as first-line kidney cancer treatment.

Belumosudil is a pill for chronic graft-versus-host disease, the long-term immune complication of donor stem-cell transplants used to cure blood cancers.

Belzutifan is the first HIF-2α inhibitor, born from Nobel-winning biology, and is now approved after kidney cancer surgery with pembrolizumab.

Binimetinib is the MEK inhibitor partnered with encorafenib; blocking the next step in the same relay stops the tumour rerouting around the BRAF block.

Bortezomib was the first proteasome inhibitor: it jams the cell's protein-recycling machine, which antibody-factory plasma cells cannot tolerate.

Bosutinib is a CML pill with less cardiovascular and pleural toxicity than its rivals; its main side effect is diarrhoea.

Brigatinib is an ALK pill with strong brain activity, approved first after crizotinib and then first line after beating it in ALTA-1L.

A pill that blocks both blood-vessel growth and the MET escape pathway, used in kidney, liver, thyroid and, since 2025, neuroendocrine cancers.

Capivasertib (Truqap) is the first AKT inhibitor, for breast cancer with PI3K-pathway mutations and, since 2026, for prostate cancer with PTEN loss.

Capmatinib is a targeted pill for the small group of lung cancers driven by a MET exon 14 skipping mutation, found by tumour sequencing.

Capmatinib and tepotinib are two pills for the roughly 3% of lung cancers with a MET exon 14 skipping mutation.

Cediranib is a tablet that blocks the blood-vessel growth signal VEGF. In alveolar soft part sarcoma, a rare very vascular sarcoma that ignores chemotherapy, a randomised trial showed it shrinks tumours and delays progression, although it was never licensed.

Ceritinib is a second-generation ALK pill for lung cancer, effective after crizotinib but with gastrointestinal toxicity that limited uptake.

Cobimetinib is the MEK partner for vemurafenib, and the first drug approved for histiocytic neoplasms.

Copanlisib is an intravenous PI3K inhibitor for relapsed follicular lymphoma, approved in 2017 and withdrawn in 2023 when its confirmatory trial failed.

Crizotinib was the first ALK inhibitor, approved four years after ALK fusions were found in lung cancer; it was also the first drug for ROS1 lung cancer and for ALK-positive lymphoma and inflammatory myofibroblastic tumour in children.

Dabrafenib (Tafinlar) is a capsule that switches off the faulty BRAF protein driving some melanomas, lung, thyroid and other cancers. It is almost always paired with trametinib.

Dabrafenib plus trametinib is the BRAF-plus-MEK pill combination, approved for BRAF V600E lung cancer and, since 2022, for any solid tumour with that mutation.

A second-generation EGFR pill that beat gefitinib on survival in EGFR-mutant lung cancer but was quickly overshadowed by osimertinib.

Dalpiciclib is Hengrui's CDK4/6 inhibitor, the first China-developed drug of the class, approved for hormone-driven advanced breast cancer on the DAWNA trials.

Dasatinib is a second-generation BCR::ABL1 pill that, combined with the immunotherapy blinatumomab, can put Ph-positive ALL into deep remission with no chemotherapy at all.

Donafenib is a Chinese redesign of sorafenib that lived longer than the original in a head-to-head liver cancer trial and is approved in China as a first-line option.

A dual PI3K inhibitor for relapsed CLL whose survival data raised FDA concern; use is now limited to late lines.

Elraglusib blocks a kinase that helps pancreatic cancer resist chemotherapy; in a randomised phase 2 it lengthened survival when added to gemcitabine and nab-paclitaxel, and a phase 3 is planned.

Encorafenib is a BRAF inhibitor that, with cetuximab and chemotherapy, became first-line standard for BRAF-mutant colorectal cancer in 2026.

A Chinese-developed ALK pill approved in the US in December 2024 for first-line ALK-positive lung cancer.

Entrectinib (Rozlytrek) is a pill for NTRK-fusion cancers and ROS1 lung cancer that reaches brain metastases.

The first targeted pill for bladder cancer, for the roughly 20% of tumours with FGFR3 alterations, used after immunotherapy.

Erlotinib was one of the first EGFR pills for lung cancer; it was approved before anyone knew EGFR mutations predicted who would respond, then redefined by them.

An mTOR-blocking pill that doubled progression-free time with exemestane in 2012 and is now paired with the oral SERD giredestrant.

A second JAK inhibitor for myelofibrosis that works after ruxolitinib fails; it carries a boxed warning for a rare brain toxicity (Wernicke encephalopathy) so thiamine is checked.

Flumatinib is Hansoh Pharma's second-generation BCR-ABL inhibitor, approved in China in 2019 for newly diagnosed chronic-phase chronic myeloid leukaemia.

Fostamatinib is a tablet that blocks the enzyme SYK so the spleen stops destroying antibody-coated platelets; it is approved for chronic immune thrombocytopenia and was first trialled as a lymphoma drug.

A Chinese-discovered pill that blocks the blood-vessel receptors, approved in 2023 for bowel cancer after all standard treatments.

Fulzerasib was the first KRAS G12C-blocking pill approved in China, for lung cancers carrying that mutation after earlier treatment.

Furmonertinib is a Chinese lung cancer pill of the same class as osimertinib, which more than doubled the time before cancer grew compared with gefitinib in the FURLONG trial.

Futibatinib is a covalent FGFR inhibitor for FGFR2-fusion bile duct cancer, with the highest response rate of the first-generation drugs.

Garsorasib is InventisBio's KRAS G12C-blocking pill, approved in China in 2024 for previously treated lung cancer with that mutation.

An intravenous drug that blocks the whole PI3K/mTOR pathway, approved in July 2026 for hormone-positive breast cancer.

The lung-cancer pill whose dramatic responses in a few patients led to the discovery of EGFR mutations in 2004.

A single pill that beats salvage chemotherapy for relapsed FLT3-mutated AML, and the backbone of the triplets now being tested in frontline disease.

Glasdegib is a hedgehog-pathway pill that, with low-dose chemotherapy, extends survival in older AML patients who cannot have intensive treatment; it has largely been displaced by venetoclax combinations.

Glecirasib is Jacobio's KRAS G12C inhibitor, approved in China in 2024 for previously treated non-small cell lung cancer with that mutation, and in a phase 3 trial against docetaxel.

Glumetinib is a Chinese MET inhibitor approved in 2023 for lung cancers with MET exon 14 skipping, one of three such drugs approved in China and now in a phase 3 trial in gastric cancer.

Golidocitinib is Dizal's JAK1 inhibitor, approved in China in 2024 as the first JAK inhibitor for relapsed peripheral T-cell lymphoma, a cancer with few options after first-line chemotherapy.

GSK2256098 is a tablet that blocks an enzyme called FAK, which meningiomas missing the NF2 gene rely on. In the Alliance A071401 trial it slowed progression in recurrent NF2-mutant meningiomas, one of the first positive results for a targeted drug in this tumour.

The pill that ended chemotherapy for most CLL. It blocks the survival signal B cells depend on, and it was the first drug to beat chemoimmunotherapy in nearly every CLL setting.

Icotinib, approved in 2011, was the first cancer drug invented and developed in China, and it showed that a domestic lung cancer pill could match a Western one head to head.

Idelalisib was the first PI3K inhibitor for blood cancers; it is effective in CLL with rituximab but so toxic (colitis, hepatitis, pneumonitis, infections) that the class has largely been abandoned.

The drug that started the targeted therapy era in 2001, turning chronic myeloid leukaemia into a manageable condition with near-normal life expectancy.

Inavolisib is a PI3K drug that also destroys the mutant protein, approved in 2024 with palbociclib and fulvestrant for PIK3CA-mutant breast cancer.

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.

Iruplinalkib is Qilu Pharmaceutical's second-generation ALK inhibitor, approved in China in 2023 for ALK-positive non-small-cell lung cancer after crizotinib and in 2024 as first-line treatment.

The first drug to block a mutant metabolic enzyme in cancer. With azacitidine it tripled survival in IDH1-mutated AML that could not take intensive chemotherapy.

Ixazomib (Ninlaro) is the first oral proteasome inhibitor for multiple myeloma, enabling an all-oral triplet with lenalidomide and dexamethasone.

Lapatinib was the first HER2-blocking pill (2007) and is now mostly a comparator arm and a late-line option, displaced by tucatinib and ADCs.

The first drug approved for a gene fusion regardless of where the cancer started; it works in about 75% of NTRK-fusion cancers, from infant fibrosarcoma to salivary and thyroid cancers.

A third-generation EGFR pill used together with amivantamab as the first regimen to beat osimertinib in EGFR-mutant lung cancer.

An oral anti-angiogenic pill that matched sorafenib in liver cancer with higher response rates, and partners with pembrolizumab in kidney and endometrial cancer.

Lerociclib is a CDK4/6 inhibitor from G1 Therapeutics developed in China by Genor Biopharma, in a phase 3 trial with letrozole for hormone receptor-positive breast cancer.

Limertinib is Aosaikang's third-generation EGFR inhibitor, approved in China in 2024 for lung cancer with the T790M resistance mutation after earlier EGFR drugs, and in phase 3 trials for first-line use.

Linperlisib is Shanghai Yingli's PI3K-delta inhibitor, approved in China in 2022 for relapsed or refractory follicular lymphoma after two or more lines.

An ALK inhibitor with the longest disease control ever recorded for a targeted lung cancer pill: 60% progression-free at five years.

The first drug to improve survival in FLT3-mutated AML, added to standard chemotherapy: median survival went from about two years to more than six.

Mirdametinib (Gomekli in the US, Ezmekly in Europe) is a MEK-blocking capsule or dispersible tablet for adults and children with neurofibromatosis type 1 whose plexiform neurofibromas cannot be removed surgically; it is the first such drug approved for adults.

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.

Momelotinib is the JAK inhibitor designed for anaemic myelofibrosis patients: it can improve haemoglobin while shrinking the spleen.

A fourth-generation ALK pill that works after lorlatinib and avoids the TRK-related brain side effects; under FDA priority review with a decision due 27 November 2026.

Nemtabrutinib is Merck's reversible BTK blocker, active against the C481S escape mutation, being tested against ibrutinib and acalabrutinib in first-line CLL.

A pill taken for a year after trastuzumab to further reduce recurrence in HER2-positive, hormone-positive breast cancer, limited by severe diarrhoea.

Nilotinib is a second-generation CML pill that produces deeper responses faster than imatinib, at the cost of cardiovascular and metabolic side effects.

Nintedanib is a triple angiokinase inhibitor pill (VEGFR, FGFR, PDGFR) approved for pulmonary fibrosis and, in the EU, for second-line lung adenocarcinoma with docetaxel. In mesothelioma the phase 2 part of LUME-Meso suggested slower progression in epithelioid disease, but the phase 3 part showed none, a much-cited warning about small randomised phase 2 signals.

Nirogacestat is the first approved medicine for desmoid tumours, locally invasive growths that do not spread but can be crippling; it works by blocking Notch signalling.

Olaratumab was approved in 2016 with doxorubicin for soft tissue sarcoma after a small trial suggested it added almost a year of life, but the large confirmatory trial found no benefit and it was withdrawn in 2019, a warning case for accelerated approvals.

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.

Olverembatinib is Ascentage Pharma's third-generation BCR-ABL inhibitor, approved in China in 2021 for chronic myeloid leukaemia carrying the T315I mutation, and now in global phase 3 trials against the established drugs; it was the one China-only approval OnCo found missing from the headline list.

Orelabrutinib is InnoCare's BTK-blocking pill for chronic lymphocytic leukaemia and mantle cell lymphoma, approved in China in 2020.

Osimertinib (Tagrisso) is the standard pill for EGFR-mutant lung cancer, now also given after surgery and with chemotherapy or after chemoradiation.

The JAK inhibitor for myelofibrosis patients whose platelet counts are too low for ruxolitinib.

Pazopanib is the only multi-kinase inhibitor approved for soft-tissue sarcoma (excluding fat-derived tumours), used after chemotherapy fails.

Pemigatinib was the first targeted therapy for bile duct cancer, for tumours with an FGFR2 gene fusion.

Pexidartinib is the first drug for tenosynovial giant cell tumour, a benign but destructive joint tumour; it is effective but has liver toxicity that requires a restricted programme.

A BTK blocker that works after the older ones stop, because it grips a different part of the enzyme. Fully approved for CLL in December 2025.

Ponatinib is the only BCR::ABL1 inhibitor that covers the T315I resistance mutation. In 2024 it became the preferred pill for newly diagnosed Ph-positive ALL.

Pralsetinib is the second selective RET pill for lung cancer, less used than selpercatinib after a change of owner and label.

Pyrotinib is an irreversible pan-ErbB kinase inhibitor pill (EGFR, HER2, HER4) from Jiangsu Hengrui, approved in China since 2018 but not in the US or EU. It is the standard HER2 pill there, given with capecitabine after trastuzumab, and the comparator that new Chinese HER2 ADCs are beating; diarrhoea affects nearly every patient.

Quizartinib is a more selective FLT3 blocker that, added to chemotherapy, roughly doubled median survival in the highest-risk FLT3 subtype.

A sorafenib successor that became the first second-line drug proven to prolong life in liver cancer (2017).

A ROS1 and NTRK pill that also works after other ROS1 drugs fail, with dizziness as its signature side effect.

A fourth-line GIST drug that locks KIT in an off state regardless of which resistance mutation the tumour has acquired.

Apatinib, sold as rivoceranib outside China, was the first pill of its kind approved for stomach cancer and is now the partner of camrelizumab in first-line liver cancer.

Ruxolitinib was the first JAK inhibitor: it shrinks the spleen and relieves symptoms in myelofibrosis and controls blood counts in polycythaemia vera, without eliminating the disease clone.

Savolitinib is a Chinese-discovered pill that blocks the MET growth signal, approved in China for lung cancers with a MET exon 14 mutation and being tested worldwide with osimertinib.

Selinexor is a first-in-class pill that traps tumour-suppressor proteins inside the nucleus; approved in myeloma, it failed its endometrial cancer test in 2026.

Selpercatinib is a selective RET inhibitor approved for any tumour with a RET fusion, with a further label update in July 2026.

Selumetinib (Koselugo) is the first medicine for children and adults with neurofibromatosis type 1 whose plexiform neurofibromas, benign but disfiguring and painful nerve tumours, cannot be removed by surgery.

Sevabertinib is an oral HER2 inhibitor for lung cancers with HER2 mutations, approved in November 2025 as an alternative to Enhertu and zongertinib.

Fyarro is an infusion of the transplant drug sirolimus packaged in albumin particles. It is the first approved treatment for malignant PEComa, a rare soft-tissue tumour driven by loss of the TSC genes.

Sonidegib (Odomzo) is the second hedgehog inhibitor for locally advanced basal cell carcinoma, similar in effect and side effects to vismodegib.

Sonrotoclax is a more potent, shorter-acting successor to venetoclax. It was approved for mantle cell lymphoma in May 2026 and is in late-stage trials with zanubrutinib for CLL.

The first drug ever to extend life in advanced liver cancer (2007), now mostly a comparator arm that newer combinations are measured against.

Sunitinib is an anti-angiogenic pill approved for pancreatic neuroendocrine tumours, kidney cancer and GIST.

An oral drug for EGFR exon 20 insertion lung cancer that succeeded where mobocertinib failed; approved in China (2023) and the US (2025).

Surufatinib is HUTCHMED's angio-immuno kinase inhibitor, approved in China in 2020 for non-pancreatic and in 2021 for pancreatic neuroendocrine tumours.

A ROS1 lung-cancer pill approved in 2025 that works in the brain and after crizotinib, with fewer dizziness-type side effects than repotrectinib.

A weekly infusion that was the first drug to extend survival in poor-risk kidney cancer (2007), and in 2024 the first targeted drug to improve outcomes in childhood rhabdomyosarcoma.

Tepotinib is a once-daily targeted pill for lung cancers driven by a MET exon 14 skipping mutation, and the MET inhibitor NICE funds in England.

A next-generation FGFR inhibitor designed to work after pemigatinib or futibatinib stop working, now in a global phase 3.

Tivozanib is a VEGF-receptor pill that hits VEGFR1 to 3 with little off-target kinase activity, so it is better tolerated than other anti-angiogenic pills, though hypertension and fatigue remain common. It is approved for kidney cancer after two or more prior treatments, and its TiNivo-2 trial showed that restarting immunotherapy after failure adds nothing.

Tovorafenib is a pill for the most common childhood brain tumour, low-grade glioma driven by BRAF changes, approved in 2024.

Trametinib (Mekinist) blocks MEK, the protein one step below BRAF in the growth-signal chain. Paired with dabrafenib it treats BRAF-mutant melanoma, lung, thyroid and other cancers, including brain tumours in children.

Trilaciclib is given as an infusion just before chemotherapy for small cell lung cancer to put the bone marrow's stem cells briefly to sleep, so fewer are killed and patients need fewer transfusions and growth factor injections.

A HER2-selective pill that works in the brain, for HER2-positive breast cancer with brain metastases.

Tunlametinib is a Chinese MEK inhibitor approved in 2024 for advanced melanoma with an NRAS mutation, a group with no targeted therapy elsewhere in the world, and in phase 3 trials with vemurafenib for BRAF-mutant disease and for colorectal cancer.

A PI3K inhibitor for marginal zone and follicular lymphoma approved in 2021 and withdrawn in 2022 after the UNITY-CLL trial suggested more deaths.

Vandetanib was the first drug approved for medullary thyroid cancer (2011), now largely replaced by RET-selective selpercatinib.

A pill that blocked the HER family of growth receptors, tested with capecitabine as second-line treatment for bile duct and gallbladder cancer. It did not beat capecitabine alone in the TreeTopp trial and development stopped.

Vebreltinib is a Chinese MET inhibitor approved in 2023 for lung cancers with a MET exon 14 skipping mutation, and the first drug tested in a phase 3 trial for glioblastomas carrying a PTPRZ1-MET fusion.

Vemurafenib was the first BRAF inhibitor (2011); it shrank melanomas in weeks and proved that a single mutation could be drugged in a solid tumour.

A pill that removes the survival shield from leukaemia cells, enabling chemotherapy-free, time-limited treatment for CLL.

Vimseltinib is a pill approved in February 2025 for tenosynovial giant cell tumour, a benign but destructive joint tumour, offering an alternative to repeated surgery.

Vismodegib was the first hedgehog-pathway drug, for basal cell carcinomas too advanced for surgery; it shrinks most tumours but muscle cramps, taste loss and hair loss make long-term use hard.

Vorolanib is Betta Pharmaceuticals' oral VEGFR and PDGFR inhibitor, approved in China in 2023 with everolimus for advanced kidney cancer after a first kinase inhibitor has failed.

Zanubrutinib is the only BTK blocker to beat ibrutinib on both efficacy and safety in a head-to-head trial. It is now the most prescribed BTK inhibitor in CLL.

A ROS1 inhibitor approved in July 2026 that works after other ROS1 drugs fail and avoids their brain side effects.

Zongertinib was the first oral HER2 inhibitor for lung cancer with HER2 mutations, approved in 2025 and moved to first line in 2026.