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Targeted agent regimens

226 articles

Capmatinib

Capmatinib (brand name Tabrecta) is an oral MET inhibitor approved in the US in May 2020, the first targeted therapy for metastatic lung cancer with MET exon 14 skipping.

Catequentinib

Catequentinib, also called anlotinib hydrochloride or AL3818, is an oral multi-target tyrosine kinase inhibitor targeting VEGFR2/3, FGFR1-4, and PDGFR; NMPA-approved in 2018 for advanced NSCLC after two chemotherapy lines.

Cediranib

Cediranib (AZD2171, RECENTIN, Zemfirza) is an oral VEGFR-1/2/3 tyrosine kinase inhibitor developed by AstraZeneca for solid tumors; it improved PFS in relapsed platinum-sensitive ovarian cancer (ICON6) but its EU marketing application was withdrawn in 2016.

Ceralasertib

Ceralasertib (AZD6738) is AstraZeneca's oral ATR kinase inhibitor for cancer, studied as monotherapy and with paclitaxel, carboplatin, olaparib, and durvalumab; the LATIFY phase III NSCLC trial missed its OS endpoint.

Ceritinib

Ceritinib (Zykadia, LDK378) is an oral second-generation ALK kinase inhibitor for ALK-positive metastatic NSCLC, FDA accelerated approval 2014, first-line 2017; dose 450 mg daily with food.

Cetuximab and encorafenib regimen

The cetuximab and encorafenib regimen pairs the EGFR antibody cetuximab with the oral BRAF V600E inhibitor encorafenib to treat BRAF V600E-mutant metastatic colorectal cancer, first FDA-approved in 2020.

Chlorambucil

Chlorambucil, sold as Leukeran, is an oral nitrogen mustard alkylating agent approved in the United States in 1957, used mainly to treat chronic lymphocytic leukemia and malignant lymphomas.

CLEAR trial

CLEAR (Study 307, NCT02811861): phase 3 trial of lenvatinib plus pembrolizumab or everolimus versus sunitinib in first-line advanced renal cell carcinoma; distinct from CLEAR Outcomes.

Cln-081

CLN-081 (zipalertinib, TAS6417) is an oral, irreversible, EGFR ex20ins-selective tyrosine kinase inhibitor for NSCLC; REZILIENT1 showed 35.2% ORR, and FDA NDA review has a February 27, 2027 PDUFA date.

Cobimetinib

Cobimetinib (Cotellic, GDC-0973, XL518), an allosteric MEK1/2 inhibitor by Exelixis and Genentech, approved 2015 with vemurafenib for BRAF V600-mutant melanoma and as single agent for histiocytic neoplasms.

Conteltinib

Conteltinib (CT-707, 康特替尼, brand 首要泽) is Shouyao Holdings' second-generation ALK/FAK/Pyk2/IGF-1R inhibitor for ALK-positive NSCLC, approved by China's NMPA on June 10, 2026 as the first granule-formulation ALK inhibitor after a phase 3 win over crizotinib.

Copanlisib

Copanlisib (Aliqopa, BAY 80-6946) is an intravenous PI3K-alpha/delta inhibitor approved by FDA in 2017 for relapsed follicular lymphoma; approval was withdrawn in March 2024 after CHRONOS-4 failed.

Cpi 613

CPI-613 (devimistat) is a lipoate-analog anticancer drug inhibiting mitochondrial PDH and alpha-ketoglutarate dehydrogenase; its phase III trials AVENGER 500 (pancreatic cancer) and ARMADA 2000 (AML) both failed their primary endpoints.

Crenolanib

Crenolanib (CP-868,596-26, crenolanib besylate) is an oral second-generation type I FLT3 and PDGFR inhibitor for FLT3-mutated AML, active against ITD and TKD mutations, not FDA-approved, with phase 3 trials versus midostaurin and in salvage therapy.

Culmerciclib capsules

Culmerciclib capsules (库莫西利胶囊, 赛坦欣) is the first approved CDK2/4/6 inhibitor, a Chia Tai Tianqing oral drug for HR+/HER2- breast cancer with fulvestrant, NMPA-approved December 2025.

Dabrafenib/trametinib regimen

The dabrafenib/trametinib regimen, also called dabrafenib and trametinib, is an oral targeted-therapy combination that blocks the MAPK pathway in BRAF V600-mutated cancers, first FDA-approved for melanoma in 2014.

Dalpiciclib

Dalpiciclib (SHR6390) is an oral CDK4/6 inhibitor from Hengrui Pharmaceuticals, approved in China in 2021, used with endocrine therapy for HR-positive/HER2-negative breast cancer; key trials include DAWNA-1, DAWNA-2, and the adjuvant DAWNA-A, with neutropenia as its characteristic toxicity.

Defactinib

Defactinib (VS-6063, PF-04554878, FAKZYNJA) is an ATP-competitive FAK/Pyk2 inhibitor (IC50 0.6 nM). FDA-approved May 2025 with avutometinib for KRAS-mutated recurrent low-grade serous ovarian cancer; failed as mesothelioma monotherapy in COMMAND.

Dinaciclib

Dinaciclib, also known as SCH 727965 or MK-7965, is an experimental anticancer drug that blocks CDK1, CDK2, CDK5, and CDK9, tested in trials without regulatory approval.

Dirozalkib

Dirozalkib (XZP-3621, Xuan Fei Ning, 地罗阿克) is Xuanzhu Biopharmaceutical's oral ALK/ROS1 inhibitor for ALK-positive advanced NSCLC; NMPA-approved August 2025 at 500 mg daily after phase 3 PFS of 29.5 months versus 12.9 with crizotinib.

DN022150 (KRAS G12D inhibitor)

DN022150 (DN-022150) is an intravenous, noncovalent small-molecule KRAS G12D inhibitor by Jiangxi Kvvit Pharmaceutical; phase I/IIa showed no DLTs and ORR up to 41.9% in pancreatic cancer, with two phase 3 trials ongoing.

Donafenib tosylate

Donafenib tosylate (甲苯磺酸多纳非尼片, Zepsun) is a Chinese-approved oral multi-kinase inhibitor related to sorafenib; first-line therapy for unresectable hepatocellular carcinoma and radioactive iodine-refractory differentiated thyroid cancer.

Dordaviprone

Dordaviprone, developed as ONC201 and sold as Modeyso, is an oral anticancer drug the FDA approved in August 2025 for H3 K27M-mutant diffuse midline glioma.

Duvelisib

Duvelisib (brand name Copiktra) is an oral inhibitor of the PI3K delta and gamma enzymes, approved in the United States in 2018 for relapsed or refractory CLL/SLL and follicular lymphoma.

EGFR-TKI therapy

EGFR-TKI therapy is drug treatment with tyrosine kinase inhibitors that block the epidermal growth factor receptor, used mainly for EGFR-mutated non-small-cell lung cancer, especially in Asian patients.

Emavusertib

Emavusertib (CA-4948, AU-4948) is Curis's oral, reversible IRAK4 kinase inhibitor, also active against FLT3 and CLK kinases, in Phase 1/2 TakeAim trials for PCNSL, AML/MDS, and CLL.

Enasidenib

Enasidenib (Idhifa, AG-221) is an oral first-in-class mutant IDH2 inhibitor approved in the US in 2017 for relapsed/refractory IDH2-mutant AML; it lowers 2-HG, induces differentiation, and carries a differentiation syndrome boxed warning.

Encorafenib plus binimetinib

Encorafenib plus binimetinib is an oral targeted-therapy regimen combining a BRAF and a MEK inhibitor, approved in the United States in 2018 for BRAF V600-mutant melanoma.

Ensartinib

Ensartinib (Ensacove, X-396, Beimeina) is a second-generation ALK/ROS1/MET kinase inhibitor for ALK-positive NSCLC; FDA-approved December 18, 2024 at 225 mg daily, with eXalt3 and ELEVATE trial evidence.

Entinostat

Entinostat (MS-275, SNDX-275) is an oral class I-selective benzamide HDAC inhibitor (HDAC1/HDAC3) studied in breast cancer and other tumors; approved in China in 2024, with PFS benefit but no overall survival gain in meta-analysis.