Clinical Trials

Numerous clinical trials spanning Phase I through Phase III have evaluated galunisertib (LY2157299) as monotherapy and combination regimens in healthy volunteers and across conditions including glioblastoma, myelodysplastic syndromes, and metastatic pancreatic, recurrent hepatocellular, colorectal, and prostate cancers. Spearheaded by industry sponsor Eli Lilly and Company alongside academic collaborators, these studies encompass recruitment statuses ranging from active and recruiting to completed or withdrawn.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07321860 NOT_YET_RECRUITING
ALS (Amyotrophic Lateral Sclerosis)
Gipfel Life Sciences GmbH
 2026-06-30 PHASE2; PHASE3
NCT05700656 ACTIVE_NOT_RECRUITING
Colorectal Cancer Metastatic; Peritoneal Carcinomatosis
The Netherlands Cancer Institute
 2023-07-28 PHASE1; PHASE2
NCT04605562 NOT_YET_RECRUITING
Nasopharyngeal Carcinoma
Sun Yat-sen University
 2022-06 PHASE2
NCT02688712 ACTIVE_NOT_RECRUITING
Rectal Adenocarcinoma
Providence Health & Services
 2016-03-24 PHASE2
NCT02452008 ACTIVE_NOT_RECRUITING
Prostate Cancer
Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins
 2016-05-03 PHASE2
NCT03206177 COMPLETED
Carcinosarcoma, Ovarian
University of Oklahoma
 2017-08-23 PHASE1
NCT02906397 COMPLETED
ADVANCED HEPATOCELLULAR CARCINOMA (HCC)
Abramson Cancer Center at Penn Medicine
 2017-03-30 PHASE1
NCT02672475 COMPLETED
Estrogen Receptor Negative; HER2/Neu Negative; Progesterone Receptor Negative; Recurrent Breast Carcinoma; Stage IV Breast Cancer; Triple-Negative Breast Carcinoma
Vanderbilt-Ingram Cancer Center
 2016-03 PHASE1
NCT03470350 WITHDRAWN
Colorectal Cancer Metastatic
The Netherlands Cancer Institute
 2018-08-24 PHASE1; PHASE2
NCT04031872 Unknown status
Colorectal Cancer Metastatic
The Netherlands Cancer Institute|Vall d''Hebron Institute of Oncology|Agendia|European Organisation for Research and Treatment of Cancer - EORTC|Azienda Ospedaliera Niguarda Cà Granda|Fundación para la Investigación del Hospital Clínico de Valencia|University of Campania Luigi Vanvitelli|University of Turin Italy|Eli Lilly and Company|Catalan Institute of Health|Universitaire Ziekenhuizen KU Leuven
 2020-02 Phase 1|Phase 2
NCT01246986 COMPLETED
Carcinoma, Hepatocellular
Eli Lilly and Company
 2011-03-30 PHASE2
NCT02423343 COMPLETED
Solid Tumor; Non-Small Cell Lung Cancer Recurrent; Hepatocellular Carcinoma Recurrent
Eli Lilly and Company
 2015-01-01 PHASE1; PHASE2
NCT02538471 TERMINATED
Metastatic Breast Cancer
Weill Medical College of Cornell University
 2015-08-10 PHASE2
NCT02734160 COMPLETED
Metastatic Pancreatic Cancer
Eli Lilly and Company
 2016-06-15 PHASE1
NCT03470350 Withdrawn
Colorectal Cancer Metastatic
The Netherlands Cancer Institute|Vall d''Hebron Institute of Oncology|Agendia|European Organisation for Research and Treatment of Cancer - EORTC|Azienda Ospedaliera Niguarda Cà Granda|Fundación para la Investigación del Hospital Clínico de Valencia|University of Campania Luigi Vanvitelli|University of Turin Italy|Eli Lilly and Company|Catalan Institute of Health|Universitaire Ziekenhuizen KU Leuven
 2018-08-24 Phase 1|Phase 2
NCT02240433 COMPLETED
Hepatocellular Carcinoma
Eli Lilly and Company
 2014-11-12 PHASE1
NCT02178358 COMPLETED
Hepatocellular Carcinoma
Eli Lilly and Company
 2014-08-08 PHASE2
NCT02304419 COMPLETED
Neoplasm
Eli Lilly and Company
 2015-05 PHASE1
NCT02734160 Completed
Metastatic Pancreatic Cancer
Eli Lilly and Company|AstraZeneca
 2016-06-15 Phase 1
NCT02752919 COMPLETED
Healthy
Eli Lilly and Company
 2016-04 PHASE1
NCT02452008 Recruiting
Prostate Cancer
Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Eli Lilly and Company
 2016-05-03 Phase 2
NCT02752919 Completed
Healthy
Eli Lilly and Company
 2016-04 Phase 1
NCT02008318 COMPLETED
Myelodysplastic Syndromes
Eli Lilly and Company
 2014-03 PHASE2; PHASE3
NCT01373164 COMPLETED
Neoplasms; Neoplasm Metastasis; Pancreatic Cancer
Eli Lilly and Company
 2011-06 PHASE1; PHASE2
NCT01220271 COMPLETED
Glioma
Eli Lilly and Company
 2011-04 PHASE1; PHASE2
NCT02154646 COMPLETED
Pancreatic Neoplasms
Eli Lilly and Company
 2014-05 PHASE1
NCT01582269 COMPLETED
Glioblastoma
Eli Lilly and Company
 2012-04-26 PHASE2
NCT01722825 COMPLETED
Neoplasms; Neoplasm Metastasis
Eli Lilly and Company
 2012-11 PHASE1
NCT01965808 COMPLETED
Healthy Volunteers
Eli Lilly and Company
 2013-10 PHASE1
NCT01746004 COMPLETED
Healthy Volunteers
Eli Lilly and Company
 2013-01 PHASE1
NCT01682187 COMPLETED
Glioma
Eli Lilly and Company
 2005-12-15 PHASE1

(data from https://clinicaltrials.gov, updated on 2026-01-07)

Check the Galunisertib (LY2157299) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Galunisertib (LY2157299) selectively binds to and inhibits transforming growth factor-beta receptor I (TβRI/ALK5) kinase activity, thereby suppressing downstream phosphorylation of Smad2 and blocking canonical TGF-β signaling pathways. This molecular inhibition halts TGF-β-mediated epithelial-mesenchymal transition and tumor immunosuppression, directly impairing proliferation and invasive progression in clinical targets such as glioblastoma, pancreatic cancer, and hepatocellular 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>).

Jump to

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