Clinical Trials

Multiple clinical trials evaluate the therapeutic potential of XL888, primarily focusing on Phase 1 studies of monotherapy and combination regimens. These investigations target conditions such as advanced solid tumors, BRAF-mutated unresectable melanoma, and gastrointestinal malignancies including colorectal and pancreatic adenocarcinomas. Sponsored by academic research centers, industry partners, and the National Institutes of Health, the recruitment status across these protocols varies, encompassing completed, terminated, and active, not recruiting trials.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03095781 COMPLETED
Colorectal Adenocarcinoma; Metastatic Pancreatic Adenocarcinoma; Recurrent Colorectal Carcinoma; Recurrent Pancreatic Carcinoma; Stage III Colorectal Cancer; Stage III Pancreatic Cancer; Stage IIIA Colorectal Cancer; Stage IIIB Colorectal Cancer; Stage IV Colorectal Cancer; Stage IV Pancreatic Cancer; Stage IVA Colorectal Cancer; Stage IVA Pancreatic Cancer; Stage IVB Colorectal Cancer; Stage IVB Pancreatic Cancer; Unresectable Pancreatic Carcinoma
Emory University
2017-07-07 PHASE1
NCT02721459 ACTIVE_NOT_RECRUITING
Melanoma; Skin Cancer
H. Lee Moffitt Cancer Center and Research Institute
2016-09-07 PHASE1
NCT03095781 Completed
Colorectal Adenocarcinoma|Metastatic Pancreatic Adenocarcinoma|Recurrent Colorectal Carcinoma|Recurrent Pancreatic Carcinoma|Stage III Colorectal Cancer|Stage III Pancreatic Cancer|Stage IIIA Colorectal Cancer|Stage IIIB Colorectal Cancer|Stage IV Colorectal Cancer|Stage IV Pancreatic Cancer|Stage IVA Colorectal Cancer|Stage IVA Pancreatic Cancer|Stage IVB Colorectal Cancer|Stage IVB Pancreatic Cancer|Unresectable Pancreatic Carcinoma
Emory University|Merck Sharp & Dohme LLC|Exelixis|National Institutes of Health (NIH)|National Cancer Institute (NCI)
2017-07-07 Phase 1
NCT01657591 COMPLETED
Melanoma
H. Lee Moffitt Cancer Center and Research Institute
2012-07-27 PHASE1
NCT00796484 TERMINATED
Cancer
Exelixis
2008-11 PHASE1
NCT00796484 Terminated
Cancer
Exelixis
2008-11 Phase 1

(data from https://clinicaltrials.gov, updated on 2026-05-22)

Check the XL888 product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

XL888 functions as an ATP-competitive inhibitor of heat shock protein 90 (HSP90), binding to the chaperone to promote the degradation of oncogenic client proteins and disrupt essential oncogenic signaling cascades. This molecular destabilization induces cell cycle arrest and apoptotic cell death, driving its clinical evaluation in patients with advanced solid tumors, melanoma, and gastrointestinal malignancies.

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>).

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