Crenigacestat (LY3039478) Clinical Trials

Size	Price	Qty
5mg	USD 170
25mg	USD 570

Clinical Trials

Multiple Phase 1 and Phase 1/2 clinical trials have evaluated crenigacestat (LY3039478) in advanced solid tumors, T-cell acute lymphoblastic leukemia, T-cell lymphoblastic lymphoma, plasma cell myeloma, and healthy volunteer pharmacokinetic cohorts. Sponsored primarily by Eli Lilly and Company alongside academic partners like the Fred Hutchinson Cancer Center, these studies investigated drug safety and combination regimens. Recruitment across these documented protocols is predominantly completed, with several studies marked as terminated.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03502577	TERMINATED	Recurrent Plasma Cell Myeloma; Refractory Plasma Cell Myeloma	Fred Hutchinson Cancer Center	2018-05-23	PHASE1
NCT02836600	COMPLETED	Advanced Solid Tumor	Eli Lilly and Company	2016-09-09	PHASE1
NCT02784795	TERMINATED	Solid Tumor; Breast Cancer; Colon Cancer; Cholangiocarcinoma; Soft Tissue Sarcoma	Eli Lilly and Company	2016-11-04	PHASE1
NCT01695005	COMPLETED	Neoplasms; Neoplasm Metastasis; Lymphoma	Eli Lilly and Company	2012-10	PHASE1
NCT02518113	COMPLETED	T-cell Acute Lymphoblastic Leukemia; T-cell Lymphoblastic Lymphoma	Eli Lilly and Company	2015-10-01	PHASE1; PHASE2
NCT02906618	COMPLETED	Healthy	Eli Lilly and Company	2016-10-04	PHASE1
NCT02917733	COMPLETED	Healthy	Eli Lilly and Company	2016-09	PHASE1
NCT02906618	Completed	Healthy	Eli Lilly and Company	2016-10-04	Phase 1
NCT02917733	Completed	Healthy	Eli Lilly and Company	2016-09	Phase 1
NCT02836600	Completed	Advanced Solid Tumor	Eli Lilly and Company	2016-09-09	Phase 1
NCT02659865	COMPLETED	Healthy	Eli Lilly and Company	2016-01	PHASE1
NCT02518113	Completed	T-cell Acute Lymphoblastic Leukemia\|T-cell Lymphoblastic Lymphoma	Eli Lilly and Company	2015-10-01	Phase 1\|Phase 2

(data from https://clinicaltrials.gov, updated on 2024-01-08)

Check the Crenigacestat (LY3039478) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Crenigacestat (LY3039478) selectively binds to gamma-secretase with high potency, thereby blocking the proteolytic cleavage and subsequent nuclear translocation of Notch intracellular domain fragments. This inhibition downregulates downstream Notch target gene transcription, halting oncogenic signaling pathways and suppressing cell proliferation in Notch-dependent malignancies such as T-cell acute lymphoblastic leukemia and advanced solid tumors.

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>).