亞洲 KRAS 抑制劑
KRAS 抑制劑：關掉癌細胞裡最常卡死在「開」的生長開關。
8追蹤資產
3已核准
這個賽道在做什麼
KRAS 是一個控制細胞生長的開關，突變後會一直停在「開」的位置，在胰臟癌、大腸癌和肺癌裡特別常見。這個蛋白表面光滑、很難找到藥物卡得進去的地方，曾經被認為「打不到」。2021 年第一個 G12C 抑制劑上市後，戰場轉向更常見的 G12D、能同時壓住多種突變的泛 KRAS 藥，以及能在開啟狀態下作用的新一代分子。中國藥廠在這一波很活躍，大藥廠也開始為臨床前分子付出高額首付款。
階段分布
已核准3 3
第三期5 5
國家分布
中國7 7
日本1 1
資產表
| 排名 | 資產 | 國際非專利名稱 | 原研公司 | 國家 | 標的 | 機轉 | 最高階段 | 適應症 | 試驗登錄號 | 海外權利人 | 交易日期 | 首付款 | 總額上限 | 最新事件 | 最新事件日期 | 來源 | 來源日期 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 1 | Fulzerasib (GFH925 / IBI351; brand Dupert) | fulzerasib | GenFleet Therapeutics (Shanghai) Inc. | China | KRAS G12C | Oral KRAS G12C inhibitor | Approved — China (2024-08) | KRAS G12C NSCLC after ≥1 systemic therapy (approved Mainland China 2024-08; Macao 2025-06); CRC (CDE BTD); 1L NSCLC + cetuximab (KROCUS Ph1b/2) | NCT05005234 | NCT05756153 | Innovent Biologics (Greater China licensee); ex-China rights returned to GenFleet after option termination (Jan 2024) | 2021-09-01 | USD 22m | USD 262m (USD 22m upfront + up to USD 240m milestones; ex-China option terminated 2024-01) | GenFleet H1-2026 interim results: fulzerasib on China NRDL (Dec 2025), Macao approval (Jun 2025); USD 20m option-termination fee to Innovent being paid in instalments | 2026-08-21 | 1 2 3 4 | 2026-08-21 |
| 2 | Garsorasib (D-1553; brand An Fang Ning) | garsorasib | InventisBio Co., Ltd. | China | KRAS G12C | Oral KRAS G12C inhibitor | Approved — China (2024-11) | KRAS G12C NSCLC after ≥1 systemic therapy (approved); 2L NSCLC vs docetaxel (Ph3); 1L non-squamous NSCLC + IN10018 (Ph3) | NCT05383898 | NCT06300177 | NCT07174908 | Chia Tai Tianqing / Sino Biopharm (Mainland China licensee); no ex-China licensee reported | 2023-08 | Not disclosed | Not disclosed | Phase 3 of IN10018 + garsorasib vs PD-1 + chemo in 1L KRAS G12C non-squamous NSCLC started (sponsor InxMed) | 2025-09-10 | 1 2 3 4 5 | 2026-03-03 |
| 3 | Glecirasib (JAB-21822) | glecirasib | Jacobio Pharmaceuticals (Beijing) | China | KRAS G12C | Oral KRAS G12C inhibitor | Approved — China (2025-05) | KRAS G12C NSCLC after ≥1 systemic therapy (approved); 1L NSCLC + sitneprotafib (Ph3, CDE BTD); CRC ≥3L (Ph3 design approved); pancreatic/basket (pivotal Ph2; FDA & EMA orphan) | NCT05009329 | NCT05276726 | NCT06008288 | Allist Pharmaceuticals (Greater China licensee); Jacobio retains ex-China rights, no ex-China licensee reported | 2024-08-30 | RMB 150m (plus RMB 22.79m R&D reimbursement) | Not disclosed (RMB 50m approval milestone paid 2025) | Jacobio H1-2026 interim results: CDE Breakthrough Therapy Designation (May 2026) for glecirasib + sitneprotafib in 1L KRAS G12C NSCLC; on NRDL since Dec 2025 | 2026-08-24 | 1 2 3 4 | 2026-08-24 |
| 4 | HRS-4642 | — | Jiangsu Hengrui Pharmaceuticals | China | KRAS G12D | Selective KRAS G12D inhibitor (intravenous injection) | Phase 3 — China (2025-11) | 1L metastatic PDAC + nab-paclitaxel/gemcitabine (Ph3); perioperative PDAC (Ph3, not yet recruiting); KRAS G12D solid tumors (Ph1/2) | NCT07232875 | NCT07900789 | NCT05533463 | None reported | — | — | — | Second Phase 3 (perioperative pancreatic cancer, HRS-4642 + antitumor agents vs standard therapy) registered on ClinicalTrials.gov | 2026-10-28 | 1 2 3 4 | 2026-10-28 |
| 5 | GFH375 / VS-7375 | — | GenFleet Therapeutics (Shanghai) Inc. | China | KRAS G12D | Oral KRAS G12D (ON/OFF) inhibitor | Phase 3 — China (2025-12) | Previously treated KRAS G12D metastatic PDAC (Ph3); pretreated KRAS G12D NSCLC vs docetaxel (Ph3); both CDE BTD (H1 2026); US Ph1/2 by Verastem (FDA Fast Track) | NCT07262567 | NCT07668752 | NCT06500676 | Verastem Oncology (ex-Greater China; option exercised Jan 2025) | 2023-08-24 | USD 2m upfront (2023 option deal) + USD 6m option-exercise payment (2025-01) | Up to USD 622m (option-deal total covering up to three GenFleet programs) | Phase 3 of GFH375 vs docetaxel in pretreated KRAS G12D NSCLC started in China | 2026-07-27 | 1 2 3 4 5 | 2026-08-21 |
| 6 | Setidegrasib (ASP3082) | setidegrasib | Astellas Pharma Inc. | Japan | KRAS G12D | KRAS G12D-selective protein degrader (binds KRAS G12D and an E3 ligase) | Phase 3 — Global (2026-02) | 1L KRAS G12D metastatic PDAC + mFOLFIRINOX/NALIRIFOX (Ph3); KRAS G12D NSCLC after platinum + CPI vs docetaxel (Ph3) | NCT07409272 | NCT07566052 | NCT05382559 | None reported (in-house Astellas discovery) | — | — | — | Second Phase 3 (setidegrasib vs docetaxel in KRAS G12D NSCLC) started enrolling | 2026-04-28 | 1 2 3 | 2026-10-20 |
| 7 | HRS-7058 | — | Jiangsu Hengrui Pharmaceuticals (via subsidiary Shandong Suncadia Medicine) | China | KRAS G12C | Oral irreversible KRAS G12C (OFF-state) inhibitor | Phase 3 — China (registered 2026-05; not yet recruiting) | KRAS G12C NSCLC after standard therapy vs investigator-chosen KRAS G12C inhibitor (Ph3); pancreatic cancer (Ph2); KRAS G12C solid tumors (Ph1) | NCT07601048 | NCT07589569 | NCT06383871 | None reported | — | — | — | Phase 2 in pancreatic cancer started (after Ph3 head-to-head vs fulzerasib/garsorasib/glecirasib was registered 2026-05-22) | 2026-06-04 | 1 2 3 4 | 2026-06-11 |
| 8 | HS-10370 | — | Jiangsu Hansoh Pharmaceutical | China | KRAS G12C | Oral, highly selective small-molecule KRAS G12C inhibitor | Phase 3 — China (registered 2026-09; not yet recruiting) | 1L KRAS G12C non-squamous NSCLC + platinum doublet ± adebrelimab vs tislelizumab + chemo (Ph3); advanced solid tumors (Ph1/2, Ph1b combos) | NCT07822542 | NCT05367778 | NCT06594874 | None reported | — | — | — | Phase 3 1L NSCLC trial registered on ClinicalTrials.gov (planned start 2026-10-31) | 2026-09-16 | 1 2 | 2026-09-16 |