buparlisib
Small moleculeexperimental
Buparlisib is an experimental anti-cancer medication. It is a small molecule orally-available pan-class I phosphoinositide 3-kinase (PI3K) inhibitor. Buparlisib was under investigation as a treatment for advanced breast cancer but was abandoned due to negative results. It is still under investigation as a potential treatment for head and neck squamous cell carcinoma (HNSCC). — Wikipedia
Clinical trial activity
90 trials · 58 clinical orgs · 0 marketing orgs
Phase 1
52
Phase 2
45
Phase 3
4
Phase 4
0
Earliest trial started Nov 1, 2008 (NCT01068483)
Timeline
Indications
Studied for
- Brain Neoplasms · Phase 2
- Breast Neoplasms · Phase 3
- Carcinoma, Non-Small-Cell Lung · Phase 2
- Carcinoma, Renal Cell · Phase 1
- Carcinoma, Squamous Cell · Phase 2
- Carcinoma, Verrucous · Phase 1/Phase 2
- Cholangiocarcinoma · Phase 2
- Colonic Neoplasms · Phase 1
- Colorectal Neoplasms · Phase 2
- Drug Evaluation · Phase 1
- Drugs, Investigational · Phase 1
- Endometrial Neoplasms · Phase 2
- Esophageal Neoplasms · Phase 2
- Glioblastoma · Phase 2
- Graft vs Host Disease · Phase 1/Phase 2
- Head and Neck Neoplasms · Phase 3
- Hypopharyngeal Neoplasms · Phase 1
- Kidney Failure, Chronic · Phase 1
- Leukemia · Phase 1
- Leukemia, Lymphocytic, Chronic, B-Cell · Phase 2
- Liver Diseases · Phase 1
- Lung Neoplasms · Phase 2
- Lymphoma · Phase 2
- Lymphoma, B-Cell, Marginal Zone · Phase 1
- Lymphoma, Follicular · Phase 1
- Lymphoma, Large B-Cell, Diffuse · Phase 1
- Lymphoma, Mantle-Cell · Phase 2
- Lymphoma, Primary Cutaneous Anaplastic Large Cell · Phase 1
- Melanoma · Phase 2
- Nasopharyngeal Neoplasms · Phase 1
- Neoplasm Metastasis · Phase 2
- Neoplasms · Phase 2
- Ovarian Neoplasms · Phase 1
- Pancreatic Neoplasms · Phase 1
- Primary Myelofibrosis · Phase 1
- Prostatic Neoplasms · Phase 2
- Prostatic Neoplasms, Castration-Resistant · Phase 1
- Safety · Phase 1
- Salivary Gland Neoplasms · Phase 1/Phase 2
- Small Cell Lung Carcinoma · Phase 1
- Squamous Cell Carcinoma of Head and Neck · Phase 2
- Stomach Neoplasms · Phase 1
- Thymoma · Phase 2
- Thyroid Neoplasms · Phase 2
- Tongue Neoplasms · Phase 1/Phase 2
- Uterine Cervical Neoplasms · Phase 2
- Waldenstrom Macroglobulinemia · Phase 1
Mechanism of action
- PI3-kinase class IINHIBITOR
PI3-kinase class I inhibitor
- Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1) ↗
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (PIK3CB) ↗
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (PIK3CG) ↗
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PIK3CA) ↗
- Phosphatidylinositol 3-kinase regulatory subunit beta (PIK3R2) ↗
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PIK3CD) ↗
- Phosphoinositide 3-kinase regulatory subunit 5 (PIK3R5) ↗
- Phosphatidylinositol 3-kinase regulatory subunit gamma (PIK3R3) ↗
- PI3-kinase p85-alpha subunit
- PI3-kinase p110-delta subunit
- PI3-kinase p110-alpha subunit
- PI3-kinase p110-gamma subunit
- PI3-kinase p110-beta subunit
- PI3-kinase p85-beta subunit
- PI3-kinase p110-delta/p85-alpha
- PI3-kinase p110-alpha/p85-alpha
- PI3K p110 beta/p85 alpha
- PI3-kinase subunit gamma/Phosphoinositide 3-kinase regulatory subunit 5
- Phosphatidylinositol 3-kinase regulatory subunit beta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform/gamma isoform
- PIK3CG/PIK3R1
- Phosphatidylinositol 3-kinase regulatory subunit gamma
- Unspecified targetSupplementation
supplementation
Chemistry & pharmacology
Loading structure…
SMILES
Nc1cc(C(F)(F)F)c(-c2cc(N3CCOCC3)nc(N3CCOCC3)n2)cn1- Mol. weight
- 410.4 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaBuparlisib ↗
- ChEMBLCHEMBL2017974 ↗
Also known as
- bkm120
- bkm120
- bkm120
- bkm 120
- bkm 120
- bkm-120
- bkm-120
- bkm120-nx
- bkm120-nx
- bmk120
- buparlisib
- buparlisib
- buparlisib
- buparlisib
- buparlisib
- nvp-bkm120
- nvp-bkm120
- nvp-bkm120
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06081257 | N/A | Oct 15, 2023 | Zhejiang University |
| NCT04975958 | Phase 1 | Sep 7, 2021 | Adlai Nortye Biopharma Co., Ltd. |
| NCT04338399 | Phase 3 | Jul 31, 2020 | Adlai Nortye Biopharma Co., Ltd. |
| NCT02756247 | Phase 1 | May 1, 2016 | Cornell University, Janssen Pharmaceutica NV, Novartis |
| NCT02614508 | Phase 1 | Jan 1, 2016 | Emory University, Novartis |
| NCT01613677 | Phase 2 | Nov 1, 2015 | Novartis |
| NCT01971489 | Phase 1 | Sep 1, 2015 | National Cancer Institute (NCI), State University of New York, Buffalo |
| NCT02452294 | Phase 2 | Jul 1, 2015 | Technical University of Dresden, University of Tuebingen |
| NCT02303041 | N/A | Feb 1, 2015 | National Cancer Institute (NCI), Stanford University |
| NCT02117817 | Phase 1 | Feb 1, 2015 | National Cancer Institute (NCI), Rutgers University |
| NCT02340780 | Phase 2 | Jan 30, 2015 | Canadian Cancer Trials Group, McGill University, Novartis |
| NCT02404844 | Phase 2 | Dec 1, 2014 | iOMEDICO AG, Novartis, University of Duisburg-Essen |
| NCT02301364 | Phase 2 | Nov 20, 2014 | Cornell University, Novartis |
| NCT02113878 | Phase 1 | Oct 1, 2014 | Harvard University, Novartis |
| NCT02487823 | Phase 1 | Oct 1, 2014 | Institut Paoli-Calmettes, Novartis |
| NCT02220855 | Phase 2 | Sep 1, 2014 | Indiana University, Novartis |
| NCT01953445 | Phase 2 | Aug 1, 2014 | Washington University in St. Louis |
| NCT02049541 | Phase 1 | Jul 1, 2014 | Novartis, Ohio State University |
| NCT02194049 | Phase 1 | Jul 1, 2014 | Novartis, University of California, Davis |
| NCT02159066 | Phase 2 | Jul 1, 2014 | Array BioPharma |
Showing 20 of 90 trials
Page 1 / 5
Organizations
Research & Development (58)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Novartis | For profit | 62 | 31 | 3 | 2008 |
| Harvard University | Academic/Hospital | 8 | 7 | 2 | 2011 |
| National Cancer Institute (NCI) | Government | 8 | 0 | 3 | 2011 |
| Cornell University | Academic/Hospital | 5 | 4 | 2 | 2011 |
| SCRI Development Innovations | For profit | 3 | 3 | 1 | 2011 |
| University of California, San Francisco | Academic/Hospital | 3 | 2 | 1 | 2011 |
| Adlai Nortye Biopharma Co., Ltd. | For profit | 2 | 2 | 2 | 2020 |
| Array BioPharma | For profit | 2 | 2 | 2 | 2011 |
| Canadian Cancer Trials Group | Academic/Hospital | 2 | 2 | 1 | 2012 |
| Emory University | Academic/Hospital | 2 | 2 | 1 | 2012 |
| Institut Paoli-Calmettes | Academic/Hospital | 2 | 2 | 2 | 2011 |
| SOLTI Breast Cancer Research Group | Academic/Hospital | 2 | 1 | 1 | 2012 |
| State University of New York, Buffalo | Academic/Hospital | 2 | 2 | 1 | 2012 |
| University of North Carolina at Chapel Hill | Academic/Hospital | 2 | 2 | 1 | 2011 |
| University of Texas at Houston | Academic/Hospital | 2 | 1 | 2 | 2011 |
| University of Utah | Academic/Hospital | 2 | 1 | 1 | 2011 |
| Washington University in St. Louis | Academic/Hospital | 2 | 2 | 2 | 2011 |
| ARCAGY-GINECO | For profit | 1 | 1 | 1 | 2011 |
| AstraZeneca | For profit | 1 | 0 | 1 | 2012 |
| Cancer Research UK | Academic/Hospital | 1 | 0 | 1 | 2013 |
58 organizations
Page 1 / 3