Clinical Trials

Multiple clinical trials spanning Phase 1 through Phase 3 have evaluated entospletinib across various hematologic malignancies and immune-mediated conditions, including acute myeloid leukemia, chronic lymphocytic leukemia, diffuse large B-cell lymphoma, and chronic graft-versus-host disease. Sponsored by industry and academic entities such as Gilead Sciences, Kronos Bio, and Beat AML, LLC, these evaluations encompass completed, recruiting, and terminated protocols. Key investigations include the assessment of entospletinib in nucleophosmin 1-mutated acute myeloid leukemia.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03013998 RECRUITING
Previously Untreated Relapsed Refractory Acute Myeloid Leukemia
Beat AML, LLC
 2016-11 PHASE2; PHASE3
NCT02457598 TERMINATED
B-cell Malignancies
Gilead Sciences
 2015-06-16 PHASE1
NCT05020665 TERMINATED
Nucleophosmin 1-mutated Acute Myeloid Leukemia
Kronos Bio
 2021-11-24 PHASE3
NCT03010358 COMPLETED
Anemia; B-Cell Prolymphocytic Leukemia; Grade 1 Follicular Lymphoma; Grade 2 Follicular Lymphoma; Grade 3a Follicular Lymphoma; Hairy Cell Leukemia; Lymphoplasmacytic Lymphoma; Mantle Cell Lymphoma; Marginal Zone Lymphoma; Recurrent Chronic Lymphocytic Leukemia; Recurrent Small Lymphocytic Lymphoma; Refractory Chronic Lymphocytic Leukemia; Refractory Small Lymphocytic Lymphoma; Richter Syndrome
Alexey Danilov, MD
 2017-07-17 PHASE1; PHASE2
NCT03225924 TERMINATED
DLBCL
The Lymphoma Academic Research Organisation
 2017-07-26 PHASE1; PHASE2
NCT03135028 TERMINATED
Hematologic Malignancy; Acute Myeloid Leukemia
Gilead Sciences
 2017-05-19 PHASE1
NCT02983617 COMPLETED
Chronic Lymphocytic Leukemia
Gilead Sciences
 2017-04-06 PHASE2
NCT02404220 TERMINATED
Acute Lymphoblastic Leukemia
Gilead Sciences
 2015-05-06 PHASE1; PHASE2
NCT02343939 TERMINATED
Acute Myeloid Leukemia
Gilead Sciences
 2015-07-01 PHASE1; PHASE2
NCT02701634 TERMINATED
Chronic Graft Versus Host Disease
Gilead Sciences
 2016-05-27 PHASE2
NCT02521376 COMPLETED
Oncology
Gilead Sciences
 2015-11-16 PHASE1
NCT01799889 TERMINATED
Chronic Lymphocytic Leukemia; Mantle Cell Lymphoma; Diffuse Large B-cell Lymphoma; Non-FL Indolent Non-Hodgkin's Lymphoma; Follicular Lymphoma
Gilead Sciences
 2013-03-14 PHASE2
NCT02568683 TERMINATED
Non-Hodgkin Lymphoma
Gilead Sciences
 2016-02-11 PHASE1; PHASE2
NCT01796470 TERMINATED
Chronic Lymphocytic Leukemia; Mantle Cell Lymphoma; Diffuse Large B-cell Lymphoma; Indolent Non-Hodgkin's Lymphoma
Gilead Sciences
 2013-06-20 PHASE2
NCT01841489 COMPLETED
Chronic Lymphocytic Leukemia
Gilead Sciences
 2013-05 PHASE1

(data from https://clinicaltrials.gov, updated on 2026-09-03)

Check the Entospletinib (GS-9973) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Entospletinib acts as a selective inhibitor of spleen tyrosine kinase (Syk), binding the enzyme to block downstream protein phosphorylation and intracellular cascade propagation. This inhibition disrupts essential pro-survival signaling pathways, ultimately impairing malignant cell proliferation in clinical indications such as acute myeloid leukemia and chronic lymphocytic leukemia.

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>).

Jump to

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