prexasertib
Small moleculeexperimental
Prexasertib (LY2606368) is a small molecule checkpoint kinase inhibitor, mainly active against CHEK1, with minor activity against CHEK2. This causes induction of DNA double-strand breaks resulting in apoptosis. It was developed by Eli Lilly but the company announced in 2019 it was dropping prexasertib from active development, although clinical trials continue. Research continues into the efficacy of prexasertib in treatment of acute myeloid leukemia, myelodysplastic syndrome, rhabdomyosarcoma, and medulloblastoma. — Wikipedia
Clinical trial activity
20 trials · 12 clinical orgs · 0 marketing orgs
Phase 1
14
Phase 2
8
Phase 3
0
Phase 4
0
Earliest trial started Feb 1, 2010 (NCT01115790)
Timeline
Indications
Studied for
- Brain Neoplasms · Phase 1
- Breast Neoplasms · Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 1
- Carcinoma, Squamous Cell · Phase 1
- Carcinoma, Transitional Cell · Phase 1/Phase 2
- Central Nervous System Neoplasms · Phase 1
- Colorectal Neoplasms · Phase 1
- Desmoplastic Small Round Cell Tumor · Phase 1/Phase 2
- Endometrial Neoplasms · Phase 1/Phase 2
- Head and Neck Neoplasms · Phase 1
- Leukemia, Myeloid, Acute · Phase 1
- Leukemia, Myelomonocytic, Chronic · Phase 1
- Lung Neoplasms · Phase 1
- Medulloblastoma · Phase 1
- Myelodysplastic Syndromes · Phase 1
- Neoplasm Metastasis · Phase 1
- Neoplasms · Phase 2
- Ovarian Neoplasms · Phase 2
- Prostatic Neoplasms · Phase 2
- Rectal Neoplasms · Phase 1
- Rhabdomyosarcoma · Phase 1/Phase 2
- Small Cell Lung Carcinoma · Phase 2
- Squamous Cell Carcinoma of Head and Neck · Phase 2
- Triple Negative Breast Neoplasms · Phase 2
Mechanism of action
- Serine/threonine-protein kinase Chk1INHIBITOR
CHEK1 inhibitor
- Serine/threonine-protein kinase Chk2INHIBITOR
CHEK2 inhibitor
Selective ATP competitor inhibitor of Chk1 and Chk2 proteins
Chemistry & pharmacology
Loading structure…
SMILES
COc1cccc(OCCCN)c1-c1cc(Nc2cnc(C#N)cn2)n[nH]1- Mol. weight
- 365.4 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaPrexasertib ↗
- ChEMBLCHEMBL3545377 ↗
- ChEMBLCHEMBL3544911 ↗
Also known as
- ly2606368
- ly2606368
- ly-2606368
- ly-2606368
- prexasertib
- prexasertib
- prexasertib
- prexasertib
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06597565 | Phase 2 | Sep 25, 2024 | Acrivon Therapeutics, University of South Florida |
| NCT05548296 | Phase 1/Phase 2 (Phase 2) | Aug 29, 2022 | Acrivon Therapeutics, GOG Foundation, Inc., National Cancer Institute (NCI) |
| NCT04095221 | Phase 1/Phase 2 (Phase 2) | Sep 17, 2019 | Memorial Sloan-Kettering Cancer Center |
| NCT04023669 | Phase 1 | Aug 31, 2019 | Eli Lilly, St. Jude Children's Hospital |
| NCT04032080 | Phase 2 | Jul 31, 2019 | Baylor University, Eli Lilly |
| NCT03735446 | Phase 1 | Jan 18, 2019 | Eli Lilly, Harvard University |
| NCT03495323 | Phase 1 | May 16, 2018 | Eli Lilly, Harvard University |
| NCT03414047 | Phase 2 | Apr 10, 2018 | Eli Lilly |
| NCT03057145 | Phase 1 | Mar 10, 2017 | AstraZeneca, Dana-Farber Cancer Institute, Eli Lilly, Harvard University |
| NCT02808650 | Phase 1 | Feb 27, 2017 | National Cancer Institute (NCI) |
| NCT02873975 | Phase 2 | Oct 1, 2016 | Harvard University |
| NCT02778126 | Phase 1 | Sep 22, 2016 | Eli Lilly |
| NCT02860780 | Phase 1 | Aug 1, 2016 | Eli Lilly |
| NCT02735980 | Phase 2 | May 1, 2016 | Eli Lilly |
| NCT02649764 | Phase 1 | May 1, 2016 | Eli Lilly, University of Texas at Houston |
| NCT02555644 | Phase 1 | Feb 1, 2016 | Eli Lilly |
| NCT02514603 | Phase 1 | Oct 1, 2015 | Eli Lilly |
| NCT02203513 | Phase 2 | Jul 24, 2014 | National Cancer Institute (NCI) |
| NCT02124148 | Phase 1 | Jun 18, 2014 | Eli Lilly |
| NCT01115790 | Phase 1 | Feb 1, 2010 | Eli Lilly |
Showing 20 of 20 trials
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Organizations
Research & Development (12)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Eli Lilly | For profit | 14 | 8 | 2 | 2010 |
| Harvard University | Academic/Hospital | 4 | 3 | 2 | 2016 |
| National Cancer Institute (NCI) | Government | 3 | 2 | 2 | 2014 |
| Acrivon Therapeutics | For profit | 2 | 1 | 1 | 2022 |
| AstraZeneca | For profit | 1 | 0 | 1 | 2017 |
| Baylor University | Academic/Hospital | 1 | 1 | 1 | 2019 |
| Dana-Farber Cancer Institute | Academic/Hospital | 1 | 1 | 1 | 2017 |
| GOG Foundation, Inc. | Academic/Hospital | 1 | 0 | 1 | 2022 |
| Memorial Sloan-Kettering Cancer Center | Academic/Hospital | 1 | 1 | 1 | 2019 |
| St. Jude Children's Hospital | Academic/Hospital | 1 | 1 | 1 | 2019 |
| University of South Florida | Academic/Hospital | 1 | 1 | 1 | 2024 |
| University of Texas at Houston | Academic/Hospital | 1 | 1 | 1 | 2016 |
12 organizations
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