226 articles
A400 (RET inhibitor, KL590586)
A400 (KL590586, EP0031, lunbotinib) is an oral next-generation selective RET inhibitor from Kelun-Biotech and Ellipses Pharma for RET-altered cancers, with phase II NSCLC ORR of 81-87% and an NMPA filing in 2025.
Abexinostat
Abexinostat (PCI-24781, S78454) is an oral pan-HDAC inhibitor in trials for relapsed/refractory follicular lymphoma, showing 69.5% ORR in phase 2; not yet approved.
Abivertinib
Abivertinib (AC0010, avitinib) is an oral, irreversible, mutant-selective third-generation EGFR tyrosine kinase inhibitor for T790M-positive NSCLC, developed by Hangzhou ACEA; its phase 3 AEGIS-2 trial was withdrawn and it never reached approval.
Acalabrutinib–venetoclax regimen
The acalabrutinib–venetoclax regimen is an all-oral, chemotherapy-free combination of a BTK inhibitor and a BCL-2 inhibitor for previously untreated chronic lymphocytic leukemia, FDA-approved in 2026 after the phase 3 AMPLIFY trial.
Adagrasib
Adagrasib, sold as Krazati, is an oral KRAS G12C inhibitor developed by Mirati Therapeutics and marketed by Bristol-Myers Squibb, approved in the United States in December 2022.
Afatinib/cetuximab regimen
The afatinib/cetuximab regimen is a cancer treatment pairing oral afatinib with intravenous cetuximab to block EGFR signaling, studied in EGFR-mutant lung cancer but no longer recommended by current guidelines.
Afuresertib
Afuresertib (GSK2110183, LAE002) is an oral ATP-competitive pan-AKT inhibitor developed for cancer; phase I myeloma MTD 125 mg/day, phase III breast cancer trial AFFIRM-205 met its endpoint.
Alectinib
Alectinib (Alecensa) is an oral ALK and RET tyrosine kinase inhibitor for ALK-positive NSCLC, first approved in Japan in 2014; superior to crizotinib in ALEX and FDA-approved for adjuvant use in 2024.
Alisertib
Alisertib (MLN8237) is an investigational oral inhibitor of Aurora A kinase studied in more than 1,000 patients with blood and solid tumors, developed by Millennium Pharmaceuticals.
Alpelisib
Alpelisib, sold as Piqray and Vijoice, is an oral PI3Kα inhibitor approved by the FDA in 2019, with fulvestrant, for PIK3CA-mutated hormone receptor-positive breast cancer.
Alrizomadlin
Alrizomadlin (APG-115, AA-115) is Ascentage Pharma's oral spiro-oxindole MDM2-p53 inhibitor (IC50 3.8 nM) in phase I/II cancer trials, with six FDA orphan drug designations and no approval yet.
Andamertinib
Andamertinib (安达艾替尼, brand 安比锐) is an oral, irreversible EGFR tyrosine kinase inhibitor by Avistone for EGFR exon 20 insertion-mutant NSCLC; approved in China April 2026 after the phase 2 KANNON study showed 42.7% response rate.
Anti-EGFR therapy
Anti-EGFR therapy is a class of cancer drugs that blocks EGFR signaling, using monoclonal antibodies for colorectal cancer and tyrosine kinase inhibitors for EGFR-mutant lung cancer.
APG-2449
APG-2449 (CAS 2196186-84-0) is Ascentage Pharma's orally active FAK/ALK/ROS1 triple tyrosine kinase inhibitor, a third-generation ALK TKI with phase 1 ORR 78.6% in TKI-naive ALK+ NSCLC and two China CDE-cleared Phase III studies.
ARTS-021 (AVZO-021)
ARTS-021, renamed AVZO-021, is Allorion Therapeutics' oral selective CDK2 inhibitor licensed to Avenzo Therapeutics in 2024; in Phase 1/2 (NCT05867251) for HR+/HER2- breast cancer and CCNE1-amplified solid tumors, investigational, not FDA approved.
Asandeutertinib (TY-9591)
Asandeutertinib (TY-9591) is an oral third-generation EGFR tyrosine kinase inhibitor developed by TYK Medicines, conditionally approved in China in 2026 as first-line treatment for EGFR-mutated lung cancer with brain metastases.
Aumolertinib
Aumolertinib (almonertinib, HS-10296, Aumseqa) is a third-generation EGFR-TKI for EGFR-mutated NSCLC, approved in China in 2020; AENEAS showed median PFS 19.3 vs 9.9 months versus gefitinib, with efficacy comparable to osimertinib in indirect comparisons.
Avutometinib
Avutometinib (VS-6766, CH-5126766), a RAF/MEK clamp kinase inhibitor, is co-packaged with defactinib as Avmapki Fakzynja Co-pack, FDA-accelerated approved May 8, 2025 for KRAS-mutated recurrent low-grade serous ovarian cancer.
Balixafortide
Balixafortide (POL6326, SPX6326) is a 14-amino-acid cyclic peptide CXCR4 antagonist developed by Polyphor/Spexis via protein epitope mimetic technology; it mobilizes hematopoietic stem cells, but its phase 3 FORTRESS trial with eribulin in HER2-negative breast cancer missed its endpoints.
Barasertib
Barasertib (AZD1152) is AstraZeneca's discontinued phosphate prodrug of the selective Aurora kinase B inhibitor AZD1152-HQPA (AZD2811), studied mainly in acute myeloid leukemia before phase III failure.
Befotertinib mesylate
Befotertinib mesylate (赛美纳, D-0316/BPI-D0316) is a third-generation EGFR-TKI by Betta Pharmaceuticals for EGFR-mutated NSCLC; NMPA approved it second-line (May 2023, T790M) and first-line (October 2023), with phase 3 PFS 22.1 vs 13.8 months versus icotinib.
Bevacizumab and erlotinib combination therapy
Bevacizumab and erlotinib combination therapy, also called erlotinib and bevacizumab, is a two-drug regimen for advanced EGFR-mutated non-squamous lung cancer that prolongs progression-free survival but not overall survival.
Bewintinib
Bewintinib (OB-756, formerly Bangruitini), sold as Bangruishun, is an oral selective JAK2 inhibitor approved by China's NMPA in April 2026 for first-line treatment of intermediate-2 or high-risk myelofibrosis in adults.
BGB-43395 (CDK4 inhibitor)
BGB-43395 is an investigational oral CDK4-selective inhibitor from BeOne Medicines (formerly BeiGene) for HR+/HER2- breast cancer; phase 1 data with letrozole showed 58-68% response rates and low hematologic toxicity, and phase 3 KANDELA-302 is underway.
Binimetinib
Binimetinib (MEK162, ARRY-438162; Mektovi) is an ATP-noncompetitive MEK1/2 inhibitor by Array BioPharma, approved with encorafenib for BRAF V600-mutant melanoma; COLUMBUS PFS 14.9 vs 7.3 months.
Bireociclib tablets
Bireociclib tablets (吡洛西利), brand name Xuanyuening and research code XZP-3287, are an oral CDK4/6 inhibitor developed by Xuanzhu Biopharmaceutical and approved in China in 2025 for HR-positive, HER2-negative advanced or metastatic breast cancer.
Brivanib alaninate
Brivanib alaninate (BMS-582664) is the oral l-alanine ester prodrug of brivanib, a dual VEGFR/FGFR tyrosine kinase inhibitor developed by Bristol-Myers Squibb; its phase III HCC trials BRISK-FL and BRISK-PS missed their primary end points and the drug was never approved.
Buparlisib
Buparlisib (BKM120), Novartis oral pan-class I PI3K inhibitor; phase 3 BELLE-2/3 showed PFS benefit with fulvestrant in HR+/HER2- breast cancer but limited by rash, hyperglycemia, transaminase toxicity.
BY1298
BY1298 (BY101298, AMO-959) is Chengdu Baiyu's oral DNA-PK (PRKDC) inhibitor for solid tumors; Phase I/II in China from 2023, licensed exclusively worldwide to Novartis in October 2024 for $70 million upfront plus up to $1.1 billion in milestones.
Capivasertib
Capivasertib (Truqap, AZD5363) is AstraZeneca's first-in-class oral ATP-competitive AKT1/2/3 inhibitor, FDA-approved in 2023 with fulvestrant for PIK3CA/AKT1/PTEN-altered HR-positive HER2-negative breast cancer and in 2026 for PTEN-deficient prostate cancer.