Clinical Trials

Multiple clinical trials have evaluated grapiprant across oncology and cardiovascular indications, including non-small cell lung cancer adenocarcinoma, microsatellite stable colorectal cancer, advanced inflammatory breast carcinoma, and heart failure. Sponsored by both industry and academic institutions, including Arrys Therapeutics, Merck Sharp & Dohme LLC, M.D. Anderson Cancer Center, and Cytokinetics, these Phase 1 and combined Phase 1/2 protocols are documented as either completed or terminated.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05041101 TERMINATED
Breast Inflammatory Carcinoma; Recurrent Breast Inflammatory Carcinoma; Stage IV Breast Inflammatory Carcinoma
M.D. Anderson Cancer Center
 2021-12-21 PHASE1; PHASE2
NCT03658772 COMPLETED
Microsatellite Stable Colorectal Cancer
Arrys Therapeutics
 2018-09-20 PHASE1
NCT03696212 TERMINATED
Non-small Cell Lung Cancer Adenocarcinoma
Arrys Therapeutics
 2019-01-08 PHASE1; PHASE2
NCT03696212 Terminated
Non-small Cell Lung Cancer Adenocarcinoma
Arrys Therapeutics|Merck Sharp & Dohme LLC
 2019-01-08 Phase 1|Phase 2
NCT03658772 Completed
Microsatellite Stable Colorectal Cancer
Arrys Therapeutics|Merck Sharp & Dohme LLC
 2018-09-20 Phase 1
NCT01737866 COMPLETED
Heart Failure
Cytokinetics
 2012-11 PHASE1

(data from https://clinicaltrials.gov, updated on 2025-06-13)

Check the Grapiprant (CJ-023,423) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Grapiprant selectively binds to the prostaglandin E2 receptor subtype 4 (EP4), potently inhibiting agonist binding and suppressing downstream cyclic AMP accumulation and intracellular signaling cascades. By blocking prostaglandin E2-mediated immunosuppression and pro-inflammatory signaling, grapiprant modulates the cell microenvironment to inhibit tumor progression and inflammatory processes in targeted clinical conditions such as non-small cell lung cancer, colorectal cancer, and breast carcinoma.

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.