galunisertib
Small moleculeexperimental
Galunisertib (LY2157299) is a small molecular experimental cancer drug previously in development by Eli Lilly. It is a TGF-b inhibitor. Development of galunisertib by Eli Lilly was discontinued in January 2020. — Wikipedia
Clinical trial activity
26 trials · 22 clinical orgs · 0 marketing orgs
Phase 1
18
Phase 2
12
Phase 3
1
Phase 4
0
Earliest trial started Dec 1, 2005 (NCT01682187)
Timeline
Indications
Studied for
- Breast Neoplasms · Phase 1
- Carcinoma, Hepatocellular · Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 1/Phase 2
- Colorectal Neoplasms · Phase 2
- Glioblastoma · Phase 2
- Glioma · Phase 1/Phase 2
- Healthy Volunteers · Phase 1
- Myelodysplastic Syndromes · Phase 2/Phase 3
- Nasopharyngeal Carcinoma · Phase 2
- Neoplasm Metastasis · Phase 1/Phase 2
- Neoplasms · Phase 1/Phase 2
- Ovarian Diseases · Phase 1
- Pancreatic Neoplasms · Phase 2
- Peritoneal Neoplasms · Phase 1/Phase 2
- Prostatic Neoplasms · Phase 2
Mechanism of action
- TGF-beta receptor type IINHIBITOR
TGFBR1 inhibitor
Chemistry & pharmacology
Loading structure…
SMILES
Cc1cccc(-c2nn3c(c2-c2ccnc4ccc(C(N)=O)cc24)CCC3)n1- Mol. weight
- 369.43 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaGalunisertib ↗
- ChEMBLCHEMBL2364611 ↗
Also known as
- 4-(2-(6-methylpyridin-2-yl)-5,6-dihydro-4h-pyrrolo(1,2-b)pyrazol-3-yl)quinoline-6-carboxylic acid amide
- galunisertib
- galunisertib
- galunisertib
- galunisertib
- galunisertib
- ly2157299
- ly2157299
- ly2157299
- ly 2157299
- ly-2157299
- ly-2157299
- ly-2157299
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05700656 | Phase 1/Phase 2 (Phase 2) | Apr 30, 2023 | Netherlands Cancer Institute, University of Amsterdam |
| NCT04605562 | Phase 2 | Jun 30, 2022 | Sun Yat-Sen University |
| NCT03470350 | Phase 1/Phase 2 (Phase 2) | Aug 24, 2018 | Agendia, Catalan Institute of Health, Eli Lilly, European Organisation for Research and Treatment of Cancer, Fondazione IRCCS Cà Granda, Ospedale Maggiore Policlinico, Milano, INCLIVA, Katholieke Universiteit Leuven, Netherlands Cancer Institute, Universidad Autonoma de Barcelona, University of Campania Luigi Vanvitelli, University of Turin, University of Valencia |
| NCT03206177 | Phase 1 | Aug 20, 2017 | Eli Lilly, University of Oklahoma |
| NCT02906397 | Phase 1 | Mar 30, 2017 | University of Pennsylvania |
| NCT03081377 | Phase 1 | Mar 29, 2017 | University of Pennsylvania |
| NCT02981342 | Phase 2 | Jan 1, 2017 | Eli Lilly |
| NCT02734160 | Phase 1 | Jun 1, 2016 | AstraZeneca, Eli Lilly |
| NCT02688712 | Phase 2 | Jun 1, 2016 | Eli Lilly, Providence Health & Services |
| NCT02452008 | Phase 2 | Apr 1, 2016 | Johns Hopkins University |
| NCT02752919 | Phase 1 | Apr 1, 2016 | Eli Lilly |
| NCT02672475 | Phase 1 | Mar 1, 2016 | National Cancer Institute (NCI), Vanderbilt University |
| NCT02423343 | Phase 1/Phase 2 (Phase 2) | Oct 1, 2015 | Bristol-Myers Squibb, Eli Lilly |
| NCT02304419 | Phase 1 | May 1, 2015 | Eli Lilly |
| NCT02240433 | Phase 1 | Nov 1, 2014 | Eli Lilly |
| NCT02178358 | Phase 2 | Aug 1, 2014 | Eli Lilly |
| NCT02154646 | Phase 1 | May 1, 2014 | Eli Lilly |
| NCT02008318 | Phase 2/Phase 3 (Phase 3) | Mar 1, 2014 | Eli Lilly |
| NCT01965808 | Phase 1 | Oct 1, 2013 | Eli Lilly |
| NCT01746004 | Phase 1 | Jan 1, 2013 | Eli Lilly |
Showing 20 of 26 trials
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Organizations
Research & Development (22)
22 organizations
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