2023年欧洲内科肿瘤学（ESMO）大会将于欧洲中部夏令时间10月20日至24日以线上结合线下的形式在西班牙马德里盛启。当前ESMO官网公布的摘要内容显示，小分子靶向药物颇具治疗前景1。【肿瘤资讯】特此整理，以飨读者。
概述
Litespark-005 Ⅲ期试验于今年8月份公布：相较依维莫司，HIF-2α抑制剂Belzutifan治疗晚期肾癌患者的无进展生存期（PFS）改善，但总生存期（OS）未达到终点2。此次ESMO大会上，将公布其另一项Ⅱ期试验Litespark-013。选择性雌激素受体降解剂（SERD）OP-1250治疗HER-2阴性、ER阳性的晚期乳腺癌的OPERA-01试验即将进入Ⅲ期阶段3，其Ⅰ/Ⅱ期试验数据将于本次ESMO大会亮相。除上述之外，KRAS仍是一个具有吸引力的靶点，ESMO大会将看到Garsorasib (D-1553)、Glecirasib等新型KRASG12C抑制剂相关研究公布4（表.靶向药物相关ESMO摘要一览）。
研究及产品信息
实体瘤
摘要号及题目：1025MO - Preliminary safety, pharmacokinetics and immunomodulatory activity of RBS2418, an oral ENPP1 inhibitor, alone and in combination with pembrolizumab in patients with solid tumors
产品及机制：RBS2418；ENPP1抑制剂
企业：Riboscience
摘要号及题目：662MO - Phase 1, Multi-Center, Dose-escalation and Dose-expansion Study of IMP7068, a WEE1 Inhibitor, in Patients with Advanced Solid Tumors
产品及机制：IMP7068；WEE1 inhibitor
企业：英派药业（Impact Therapeutics）
摘要号及题目：653O - Glecirasib (KRAS G12C inhibitor) in combination with JAB-3312 (SHP2 inhibitor) in Patients with KRAS p.G12C mutated solid tumors
产品及机制：Glecirasib + JAB-3312；KRAS G12C + SHP2抑制剂
企业：加科思（Jacobio）
摘要号及题目：661MO - Anti-Tumor Activity of Belvarafenib in combination with Cobimetinib in patients with metastatic solid tumors harboring BRAF fusions or BRAF class II/III mutation
产品及机制：Belvarafenib；RAF抑制剂
企业：罗氏（Roche）
中枢神经系统肿瘤（CNS）
摘要号及题目：500O - Trotabresib (CC-90010) combined with concomitant temozolomide (TMZ) plus radiotherapy (RT) and adjuvant TMZ in patients (pts) with newly diagnosed primary glioblastoma (ndGBM): updated results from a phase 1b/2 study
产品及机制：Trotabresib (CC-90010)；BET抑制剂
企业：百时美施贵宝（Bristol Myers Squibb）
肾细胞癌（RCC）
摘要号及题目：1881O - Safety and Efficacy of Two Doses of Belzutifan in Patients (pts) With Advanced RCC: Results of the Randomized Phase 2 LITESPARK-013 Study
产品及机制：Belzutifan/Welireg；HIF-2α抑制剂
企业：默沙东（Merck & Co）
肝胆胰肿瘤
摘要号及题目：95MO - Tinengotinib in Patients with Advanced, Fibroblast Growth Factor Receptor (FGFR) inhibitor Refractory/Relapsed Cholangiocarcinoma
产品及机制：Tinengotinib；多激酶抑制剂
企业：药捷安康（南京）TransThera Sciences
肉瘤
摘要号及题目：1916MO - A first-in-human phase 1 trial of NB003, a potent and selective KIT/PDGFRa inhibitor, in patients with advanced gastrointestinal stromal tumors (GIST)
产品及机制：NB003；KIT/PDGFRa抑制剂
企业：宁波新湾（Ningbo Newbay Technology）
乳腺癌
摘要号及题目：382MO - Updated results from the phase 1/2 study of OP-1250, an oral complete estrogen receptor (ER) antagonist (CERAN) and selective ER degrader (SERD ) in patients (pts) with advanced or metastatic ER-positive, HER2-negative breast cancer
产品及机制：Palazestrant；SERD
企业：Olema
结直肠癌
摘要号及题目：550O - Safety and efficacy of D-1553 in combination with cetuximab in KRAS G12C mutated colorectal cancer (CRC): a phase II study
产品及机制：Garsorasib (D-1553)；KRAS G12C抑制剂
企业：益方生物（InventisBio）
胰腺癌及肺癌
摘要号及题目：652O - Preliminary clinical activity of RMC-6236, a first-in-class, RAS-selective, tri-complex RAS-MULTI(ON) inhibitor in patients with KRAS mutant pancreatic ductal adenocarcinoma (PDAC) and non-small cell lung cancer (NSCLC)
产品及机制：RMC-6236；RAS抑制剂
企业：Revolution
1.ESMO Congress 2023 - Conference Calendar - ESMO Congress 2023. https://cslide.ctimeetingtech.com/esmo2023/attendee/confcal/presentation/list?
2.Merck hints at progress beyond Welireg’s approved niche | ApexOnco - Clinical Trials news and analysis. https://www.oncologypipeline.com/apexonco/merck-hints-progress-beyond-weliregs-approved-niche.
3.Olema takes its antagonist/degrader concept into phase 3. https://www.oncologypipeline.com/apexonco/sites/default/files/styles/large/public/articles/breast%20cancer%20ribbon.jpg.
4.ESMO 2023 preview – a few small molecules. https://www.oncologypipeline.com/apexonco/sites/default/files/styles/large/public/articles/ESMO1.jpg.
排版编辑：肿瘤资讯-Astrid
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