Asia KRAS inhibitors
KRAS inhibitors: switching off the growth switch that is most often stuck "on" in cancer cells.
8Tracked assets
3Approved
How this track works
KRAS is a switch that controls cell growth. When it mutates it stays stuck in the "on" position, which is especially common in pancreatic, colorectal and lung cancer. The protein has a smooth surface with few pockets for a drug to grip, so it was long considered "undruggable". After the first G12C inhibitor was approved in 2021, the race moved to the more common G12D mutation, pan-KRAS drugs that block several mutations at once, and newer molecules that act on the active "on" state. Chinese companies are very active in this wave, and big pharma has started paying large upfront fees even for preclinical molecules.
Development stage
Approved3 3
Phase 35 5
Origin country / region
China7 7
Japan1 1
Assets
| Rank | Asset | INN | Originator | Country | Targets | Mechanism | Highest stage | Indication | Trial IDs | Overseas rights holder | Deal date | Upfront | Total ceiling | Latest event | Latest event date | Sources | Source date |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 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 |