Lirametostat (CPI-1205) Clinical Trials

Size	Price	Qty
2mg	USD 147
5mg	USD 270

Clinical Trials

Constellation Pharmaceuticals has sponsored several clinical trials evaluating Lirametostat (CPI-1205) across various oncology indications, all of which have completed recruitment. These Phase 1 and Phase 1b/2 studies assessed the agent in patients with B-cell lymphoma, in combination with ipilimumab for advanced solid tumors, and alongside standard anti-androgen therapies for metastatic castration-resistant prostate cancer.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03480646	COMPLETED	Metastatic Castration Resistant Prostate Cancer (mCRPC)	Constellation Pharmaceuticals	2017-11-15	PHASE1; PHASE2
NCT03525795	COMPLETED	Advanced Solid Tumors	Constellation Pharmaceuticals	2017-12-14	PHASE1
NCT02395601	COMPLETED	B-Cell Lymphoma	Constellation Pharmaceuticals	2015-03	PHASE1
NCT02395601	Completed	B-Cell Lymphoma	Constellation Pharmaceuticals	2015-03	Phase 1

(data from https://clinicaltrials.gov, updated on 2025-10-29)

Check the Lirametostat (CPI-1205) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Lirametostat (CPI-1205) functions as a selective inhibitor of the histone lysine methyltransferase EZH2 with IC50 values of 2 nM for EZH2 and 52 nM for EZH1, thereby suppressing histone H3 lysine 27 trimethylation. This inhibition reverses epigenetic gene silencing to induce cell cycle arrest and apoptosis, thereby suppressing tumor cell proliferation in clinical contexts such as B-cell lymphoma, advanced solid tumors, and metastatic castration-resistant prostate cancer.

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>).