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Targeted agent regimens

226 articles

Ibrutinib regimen

The ibrutinib regimen is a combination treatment for primary central nervous system lymphoma in which the BTK inhibitor ibrutinib is given with high-dose methotrexate, usually with rituximab.

Ibrutinib–venetoclax regimen

The ibrutinib–venetoclax regimen is an all-oral, fixed-duration therapy pairing the BTK inhibitor ibrutinib with the BCL-2 inhibitor venetoclax, used mainly for chronic lymphocytic leukemia and authorized in Europe in 2022.

Icotinib

Icotinib (埃克替尼, Conmana, BPI-2009) is an oral first-generation EGFR tyrosine kinase inhibitor developed by Betta Pharmaceuticals, approved in China in 2011 for EGFR-mutant NSCLC, with pivotal trials ICOGEN, CONVINCE, BRAIN, and EVIDENCE.

Idasanutlin

Idasanutlin (RG7388, RO5503781) is an oral Roche small-molecule MDM2 antagonist that restores p53 activity; its phase 3 MIRROS AML trial missed overall survival and development was closed in 2024.

Idelalisib

Idelalisib (Zydelig) is an oral PI3Kδ inhibitor, the first approved PI3K inhibitor, used with rituximab in relapsed CLL; its FL and SLL indications were withdrawn in 2022 over safety and poor confirmatory enrollment.

Ifebemtinib

Ifebemtinib (IN10018, BI 853520) is an oral, ATP-competitive FAK (PTK2) inhibitor developed by Boehringer Ingelheim and now InxMed, in Phase III for platinum-resistant ovarian cancer and combined with KRAS G12C inhibitors.

Ifupinostat hydrochloride for injection

Ifupinostat hydrochloride for injection (BEBT-908, CUDC-908) is an intravenous dual PI3Kα/HDAC inhibitor approved in China on 30 June 2025 for relapsed or refractory diffuse large B-cell lymphoma after two prior systemic therapies; the first dual HDAC/PI3K inhibitor approved anywhere.

Imetelstat

Imetelstat (Rytelo, GRN163L) is a first-in-class oligonucleotide telomerase inhibitor by Geron, FDA-approved June 2024 for transfusion-dependent anemia in lower-risk MDS after ESA failure; dosed 7.1 mg/kg IV every 4 weeks.

IMP1734 (PARP1-selective inhibitor)

IMP1734 (EIK1003) is a potent, highly selective PARP1 inhibitor developed by IMPACT Therapeutics and licensed to Eikon Therapeutics outside Greater China, in Phase 1/2 trials for advanced solid tumors with HRR mutations.

Infigratinib

Infigratinib (Truseltiq, BGJ398), an oral FGFR1-3 kinase inhibitor by QED Therapeutics/Helsinn, won FDA accelerated approval May 28, 2021 for FGFR2-rearranged cholangiocarcinoma (ORR 23.1%) and was withdrawn May 16, 2024.

Iniparib

Iniparib (BSI-201, SAR240550), 4-iodo-3-nitrobenzamide, an investigational anticancer drug once classed as a PARP inhibitor; promising phase 2 results in triple-negative breast cancer were not confirmed in phase 3, and it acts via cysteine-protein modification.

Ipatasertib

Ipatasertib (GDC-0068, RG7440) is Genentech's oral ATP-competitive pan-AKT1/2/3 inhibitor tested in phase III breast and prostate cancer trials; phase III results were negative and it is not approved.

Iruplinalkib

Iruplinalkib (伊鲁阿克, trade name 启欣可, code WX-0593) is Qilu Pharmaceutical's oral ALK/ROS1 tyrosine kinase inhibitor for ALK-positive NSCLC, approved in China June 2023 post-crizotinib and January 2024 first-line.

ISM3091 / XL309 (USP1 inhibitor)

ISM3091, renamed XL309, is an oral USP1 inhibitor discovered by Insilico Medicine's Chemistry42 AI platform and licensed to Exelixis for $80 million upfront in 2023; it is in a Phase 1 solid tumor trial with olaparib.

JAB-23E73, pan-KRAS inhibitor

JAB-23E73 is an investigational oral pan-KRAS inhibitor developed by Jacobio Pharmaceuticals, in phase I testing for advanced solid tumors with KRAS mutations in China and the United States.

JAB-3068

JAB-3068, an oral SHP2 (PTPN11) inhibitor by Jacobio Pharmaceuticals, entered first-in-human solid tumor trials in 2018, gained FDA orphan drug status, was licensed to AbbVie in 2020, and had development discontinued after the partnership ended.

Jaktinib hydrochloride tablets

Jaktinib hydrochloride tablets (gecacitinib, brand Zepuping, 盐酸吉卡昔替尼片) are Suzhou Zelgen's oral JAK and ACVR1 dual inhibitor, approved in China in May 2025 as the first domestic JAK inhibitor for myelofibrosis, with alopecia areata approved in 2026.

JMKX1899 (KRAS inhibitor)

JMKX1899 (JMKX001899), a Jemincare-developed oral covalent KRAS G12C inhibitor licensed ex-China to HUYABIO, binds the Switch II pocket of GDP-bound KRAS G12C and crosses the blood-brain barrier (Kpuu_CSF 0.394 in mice), in Phase I/II trials for NSCLC with brain metastases.

LAE118

LAE118 (LAE-118) is Laekna's internally discovered, orally active allosteric PI3Kα pan-mutant selective small-molecule inhibitor for PIK3CA-mutant solid tumors; FDA and China CDE IND approved, in Phase I (NCT07787520), and licensed ex-Greater China to Vasque Bio for up to USD 527 million.

Lazertinib

Lazertinib (YH25448; Leclaza, Lazcluze) is an oral, brain-penetrant third-generation EGFR tyrosine kinase inhibitor for NSCLC, approved in South Korea in 2021 and, with amivantamab, in the US in 2024.

Lenvatinib regimen

A lenvatinib regimen is an oral cancer treatment built around lenvatinib, a once-daily tyrosine kinase inhibitor given alone or with pembrolizumab, everolimus, or belzutifan for thyroid, liver, kidney, and endometrial cancers.

Lifirafenib

Lifirafenib (BGB-283) is a BeiGene/BeOne investigational pan-RAF and EGFR inhibitor for MAPK-driven tumors; phase I MTD 40 mg/day, activity in BRAF V600-mutated melanoma, thyroid, and ovarian cancers, studied with mirdametinib.

Limertinib tablets

Limertinib tablets (Aoyixin, 奥壹新; ASK120067) are a third-generation EGFR tyrosine kinase inhibitor approved in China in 2025 for T790M-mutated and first-line EGFR-mutated NSCLC, with phase 3 PFS of 20.7 months versus gefitinib.

Linifanib

Linifanib (ABT-869), an oral VEGF/PDGF receptor tyrosine kinase inhibitor developed by Abbott for cancer; its phase III HCC trial against sorafenib failed the overall survival primary endpoint (9.1 vs 9.8 months).

Linperlisib

Linperlisib (林普利塞; development code YY-20394) is an oral, selective PI3K delta inhibitor developed by Shanghai Yingli Pharmaceutical and conditionally approved in China in 2022 for relapsed or refractory follicular lymphoma.

Linsitinib

Linsitinib (OSI-906, ASP-7487, VGN-001) is an oral dual IGF-1R/insulin receptor kinase inhibitor (IC50 35/75 nM) that failed phase 3 in adrenocortical carcinoma and is now in phase 3 for thyroid eye disease.

Lisaftoclax tablets

Lisaftoclax (利沙托克拉, brand Lisengtuo 利生妥, APG-2575) is Ascentage Pharma's oral Bcl-2 inhibitor, conditionally approved in China July 2025 for previously treated CLL/SLL; second Bcl-2 inhibitor marketed globally.

Luvometinib tablets

Luvometinib tablets (芦沃美替尼片, Fumaiming, FCN-159) is Fosun Pharma's oral MEK1/2 inhibitor, a Chinese class 1 drug approved May 2025 for adult LCH/histiocytic neoplasms and pediatric NF1 plexiform neurofibromas.

Mefatinib maleate tablets (美凡厄替尼)

Mefatinib maleate tablets (美凡厄替尼, trade name 迈瑞东, mifanertinib maleate, MET-306) is an NMPA-approved Class 1 irreversible EGFR/HER2 inhibitor for first-line EGFR L858R NSCLC, approved October 2025 after a phase III head-to-head win over gefitinib.

Midostaurin

Midostaurin (Rydapt) is an oral multikinase inhibitor derived from staurosporine, approved in 2017 as the first targeted treatment for FLT3-mutated acute myeloid leukemia and for advanced systemic mastocytosis.