Clinical Trials

Multiple clinical trials across Phase 1 to Phase 3 are evaluating setidegrasib (ASP3082) in KRAS G12D-mutated advanced solid tumors, locally advanced or metastatic non-small cell lung cancer (NSCLC), and metastatic pancreatic ductal adenocarcinoma, alongside pharmacokinetic assessments in healthy volunteers. Sponsored by Astellas Pharma and Gustave Roussy, recruitment across these studies ranges from active and recruiting to not yet recruiting. Key research includes a Phase 1 trial in solid tumors, a Phase 3 trial comparing setidegrasib to docetaxel in NSCLC, and a Phase 3 trial evaluating setidegrasib with chemotherapy in pancreatic cancer.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07566052 RECRUITING
Non-small Cell Lung Cancer (NSCLC)
Astellas Pharma Global Development, Inc.
 2026-04-28 PHASE3
NCT07409272 RECRUITING
Pancreatic Cancer; Metastatic Pancreatic Cancer; Metastatic Pancreatic Adenocarcinoma
Astellas Pharma Global Development, Inc.
 2026-02-17 PHASE3
NCT05382559 RECRUITING
Solid Tumor
Astellas Pharma Inc
 2022-06-08 PHASE1
NCT07483983 RECRUITING
Metastatic/Locally Advanced Non-Small-Cell Lung Cancer; Metastatic/Locally Pancreatic Ductal Adenocarcinoma
Gustave Roussy, Cancer Campus, Grand Paris
 2026-03-25 PHASE2
NCT07395024 ACTIVE_NOT_RECRUITING
Healthy Volunteer
Astellas Pharma Global Development, Inc.
 2026-02-03 PHASE1
NCT07773129 NOT_YET_RECRUITING
Healthy Volunteer
Astellas Pharma Global Development, Inc.
 2026-08-31 PHASE1

(data from https://clinicaltrials.gov, updated on 2026-09-02)

Check the Setidegrasib (ASP3082) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Setidegrasib (ASP3082) is a proteolysis targeting chimera (PROTAC) degrader that selectively binds mutant KRAS G12D protein and recruits E3 ubiquitin ligase to induce targeted proteasomal degradation, thereby blocking downstream oncogenic signaling cascades and suppressing tumor cell proliferation. By inhibiting KRAS G12D-mediated cell survival pathways, setidegrasib induces targeted tumor growth inhibition, supporting its therapeutic evaluation in KRAS G12D-mutated malignancies such as non-small cell lung cancer and pancreatic adenocarcinoma.

Appendix RUO and cGMP Quality Standards

Quality Dimension RUO (Research Use Only) cGMP (Current Good Manufacturing Practice)
Clinical Applicability Prohibited in human clinical trials or medical diagnostics. Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status Non-regulated grade; exempt from drug manufacturing laws. Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment Unclassified analytical or research laboratories. Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control Basic purity and activity testing. Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation Basic equipment calibration; no process validation required. Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance Vendor self-declared without required formal QMS. Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact High risk of IND rejection if used as a critical raw material. Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).

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Note: Technical data last updated: Sep 1, 2026.