预约演示
更新于：2026-10-03
D3S-001
更新于：2026-10-03
概要
基本信息
原研机构 |
在研机构 |
非在研机构- |
权益机构- |
最高研发阶段临床2期 |
首次获批日期- |
最高研发阶段(中国)临床2期 |
特殊审评快速通道 (美国)、孤儿药 (美国)、突破性疗法 (中国)、突破性疗法 (美国) |
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结构/序列
分子式C32H35F6N7O3 |
InChIKeyJOLORSRKBHXPFT-PNGHJTAWSA-N |
CAS号2914919-85-8 |
关联
4
项与 D3S-001 相关的临床试验NCT07093398
A Phase 1 Open-label, Randomised, Crossover Study to Assess the Effect of Food on the Pharmacokinetics (PK) of D3S-001 in Healthy Adult Participants
CTR20250246
一项在健康参与者中评估D3S-001 以两种不同生产工艺制备的胶囊给药后相对生物利用度的随机、开放、双周期交叉1 期临床研究
NCT05886920
A Phase 1/2, Open Label, Dose-escalation, and Dose-expansion Study Evaluating the Safety, Tolerability, Pharmacokinetics, and Recommended Phase 2 Dose of D3S-002 Monotherapy or Combination Therapy in Adult Subjects With Advanced Solid Tumors With MAPK Pathway Mutations
100 项与 D3S-001 相关的临床结果
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100 项与 D3S-001 相关的转化医学
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100 项与 D3S-001 相关的专利（医药）
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4
项与 D3S-001 相关的文献（医药）2026-06-01Cancer Discovery
Elisrasib Elicits Clinical Benefit in KRASG12C-mutant NSCLC
Article
Abstract::
In a phase I/II clinical trial, patients with locally advanced or metastatic KRAS G12C-mutant non–small cell lung cancer treated with the next-generation KRASG12C inhibitor elisrasib showed robust and durable clinical responses. Patients naïve to KRASG12C inhibitors, as well as those refractory to other such drugs, experienced high rates of disease control—98.5% and 83.9%, respectively.
2026-03-01CANCER GENE THERAPY
Therapeutic advances with KRASG12C inhibitors and combination strategies in non-small cell lung cancer brain metastases
Review
作者: Bhattacharya, Debanjan ; Roman, Benjamin ; Reddy, Sanjana
Abstract:
Non-small cell lung cancer (NSCLC) frequently metastasizes to the brain in approximately 20–40% of cases. Mutations in the Kirsten rat sarcoma viral oncogene homologue (KRAS) are common in NSCLC, with the KRAS
G12C
variant accounting for approximately 40% of KRAS-mutant cases. Up to 40% of NSCLC patients harboring the KRAS
G12C
mutation develop brain metastases during follow-up, and a substantial proportion present with brain metastases at diagnosis. While KRAS
G12C
inhibitors such as sotorasib and adagrasib are approved therapies, most patients with KRAS
G12C
mutant NSCLC experience disease progression within 5 to 6 months. Emerging KRAS
G12C
inhibitors, such as adagrasib, RMC-6236, and olomorasib, show intracranial activity in KRAS
G12C
mutant NSCLC brain metastases, but adaptive resistance limits their effectiveness as monotherapies. This article examines the clinical and translational application of specific next-generation blood-brain barrier penetrant KRAS
G12C
inhibitors, such as sotorasib, adagrasib, olomorasib, RMC-6236, and D3S-001, and their rational integration with radiation therapy, targeted therapies, and immunotherapies to overcome therapeutic resistance in patients with NSCLC brain metastases. This review summarizes recent advances aimed at enhancing intracranial tumor control and overall survival in patients with NSCLC brain metastases through the use of next-generation KRAS
G12C
inhibitors and multimodal therapies.
2025-08-01NATURE MEDICINE
D3S-001 in advanced solid tumors with KRASG12C mutations: a phase 1 trial
Article
作者: Jun Zhao ; Qian Chen ; Jia Wang ; Zhi Jian Chen ; Anwen Liu ; Jun Zhang ; Zifei Fan ; Zhengbo Song ; Herbert H. Loong ; Melissa L. Johnson ; Yandong Shen ; Byoung Chul Cho ; Gary Richardson ; Myung Ah Lee ; Tony Mok ; Jing Zhang ; John J. Park ; Sun Min Lim ; Yanqiao Zhang ; Shun Lu ; Hui Wang ; Cheng Chen ; Ziming Li
D3S-001 is a next-generation KRAS-G12C inhibitor (G12Ci) designed to enhance target engagement efficiency and overcome growth factor-induced nucleotide exchange. D3S-001 was evaluated in a phase 1a dose-escalation study in patients with advanced solid tumors harboring KRASG12C mutation (N = 42) and a phase 1b expansion cohort of patients with non-small-cell lung cancer (NSCLC) whose disease progressed after prior G12Ci therapy (N = 20). The primary endpoints were safety and determination of the maximum tolerated dose. Secondary endpoints included pharmacokinetics, confirmed objective response rate (ORR) and disease control rate. D3S-001 demonstrated dose-dependent pharmacokinetics and no dose-limiting toxicities, and the maximum tolerated dose was not reached. Grade 3 treatment-related adverse events were reported in seven patients (16.7%) in the G12Ci-naive dose-escalation cohort and two patients (10.0%) in the G12Ci-pretreated NSCLC expansion cohort. There were no grade 4 or 5 treatment-related adverse events. D3S-001 600 mg was selected as the dose for further investigation based on pharmacokinetics. Confirmed ORR in the G12Ci-naive population was 73.5% overall (25 of 34), and 66.7% (14 of 21), 88.9% (8 of 9) and 75.0% (3 of 4) in patients with NSCLC, colorectal cancer and pancreatic ductal adenocarcinoma, respectively. Among patients with G12Ci-pretreated NSCLC, ORR was 30.0% (6 of 20) and disease control rate was 80.0% (16 of 20). This study demonstrates the safety and tolerability of D3S-001 monotherapy with promising antitumor activity. The phase 1b expansion phase is ongoing. ClinicalTrials.gov identifier: NCT05410145 .
100 项与 D3S-001 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D13352 | - | - | - |
研发状态
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| KRAS G12C突变的实体瘤 | 临床2期 | 美国 | 2022-08-03 | |
| KRAS G12C突变的实体瘤 | 临床2期 | 澳大利亚 | 2022-08-03 | |
| KRAS G12C突变的实体瘤 | 临床2期 | 法国 | 2022-08-03 | |
| KRAS G12C突变的实体瘤 | 临床2期 | 德国 | 2022-08-03 | |
| KRAS G12C突变的实体瘤 | 临床2期 | 意大利 | 2022-08-03 | |
| KRAS G12C突变的实体瘤 | 临床2期 | 韩国 | 2022-08-03 | |
| KRAS G12C突变的实体瘤 | 临床2期 | 西班牙 | 2022-08-03 | |
| 局部晚期恶性实体瘤 | 临床2期 | 美国 | 2022-08-03 | |
| 局部晚期恶性实体瘤 | 临床2期 | 中国 | 2022-08-03 | |
| 局部晚期恶性实体瘤 | 临床2期 | 日本 | 2022-08-03 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1/2期 | 95 | 衊簾壓齋構蓋選膚遞願(顧壓顧鏇選簾廠醖蓋鏇) = 憲餘鹹膚願廠齋鏇遞艱 簾網構顧鏇憲艱壓艱壓 (遞製膚襯網範窪艱蓋蓋 ) 更多 | 积极 | 2026-05-29 | |||
衊簾壓齋構蓋選膚遞願(顧壓顧鏇選簾廠醖蓋鏇) = 範網觸獵廠醖艱觸膚醖 簾網構顧鏇憲艱壓艱壓 (遞製膚襯網範窪艱蓋蓋 ) 更多 | |||||||
临床1/2期 | 101 | (CRC) | 鹹鹽鏇範糧顧壓艱淵鹽(廠衊艱壓積糧餘齋選膚) = 觸製襯鹽簾蓋簾願繭壓 顧廠鹽願齋鹽顧願網選 (襯膚鏇築鹹築艱夢淵憲 ) 更多 | 积极 | 2026-04-21 | ||
(PDAC) | 鹹鹽鏇範糧顧壓艱淵鹽(廠衊艱壓積糧餘齋選膚) = 醖繭願衊鏇構糧餘憲衊 顧廠鹽願齋鹽顧願網選 (襯膚鏇築鹹築艱夢淵憲 ) 更多 | ||||||
临床1期 | 62 | (phase 1a；solid tumors) | 夢遞製鹹憲遞築夢窪簾(廠淵襯糧艱鹽築醖鏇淵) = 蓋壓獵簾遞願製選蓋壓 範壓築繭願顧鹽餘廠簾 (鑰淵衊繭顧糧齋窪鏇齋 ) 更多 | 积极 | 2025-04-29 | ||
(phase 1a；G12Ci-naive NSCLC) | 憲蓋襯觸餘夢遞築鬱齋(獵選鹽鑰夢廠鹹鑰製淵) = 網壓遞鹽糧壓糧齋夢遞 憲壓淵蓋齋鬱蓋窪遞獵 (膚廠鹽願鹹顧餘選範簾 ) | ||||||
临床2期 | 20 | 範遞膚構鏇壓顧築範憲(糧築淵襯廠積願鹹願艱) = 繭遞顧範夢製鏇築繭齋 廠壓夢衊繭鏇製願蓋窪 (築膚淵廠選簾築繭壓製 ) 更多 | 积极 | 2025-04-29 | |||
临床1/2期 | 42 | D3S-001 50 mg | 醖廠構衊窪觸積蓋鑰獵(壓築憲廠網鹽簾鏇艱衊) = 簾顧糧鹹選鹽糧網鑰鏇 衊觸觸膚衊醖鏇構遞願 (齋夢鹽窪繭齋簾齋遞艱 ) 更多 | 积极 | 2024-09-14 | ||
(G12Ci naïve) | 鹹構願遞選艱鹹鏇糧壓(製鹹獵壓網衊鑰蓋廠遞) = 鏇艱網夢壓夢餘糧憲願 夢廠鬱鹹憲繭構鹹鏇繭 (築廠齋蓋顧顧網糧膚簾 ) 更多 | ||||||
临床1期 | KRAS G12C突变的实体瘤 KRAS G12C | 41 | 網夢膚積艱鏇廠獵簾遞(窪積簾觸廠憲構網鏇夢) = 蓋餘鏇築糧蓋夢廠壓膚 夢鏇獵襯網築膚網壓積 (築顧獵網鹽鹹淵壓鬱製 ) 更多 | 积极 | 2024-04-05 |
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