dactolisib
Small moleculeexperimental
Dactolisib is an imidazoquinoline derivative acting as a PI3K inhibitor. It also inhibits mTOR. It is being investigated as a possible cancer treatment. — Wikipedia
Clinical trial activity
23 trials · 11 clinical orgs · 0 marketing orgs
Phase 1
14
Phase 2
13
Phase 3
2
Phase 4
0
Earliest trial started Dec 21, 2006 (NCT00620594)
Timeline
Indications
Studied for
- Breast Neoplasms · Phase 2
- Carcinoma, Renal Cell · Phase 1
- Carcinoma, Transitional Cell · Phase 2
- Endometrial Neoplasms · Phase 2
- Hamartoma Syndrome, Multiple · Phase 1
- Kidney Neoplasms · Phase 1/Phase 2
- Leukemia, Myeloid, Acute · Phase 1
- Leukemia, Myeloid, Chronic-Phase · Phase 1
- Lung Diseases · Phase 3
- Neoplasm Metastasis · Phase 2
- Neoplasms · Phase 1/Phase 2
- Pancreatic Neoplasms · Phase 2
- Precursor Cell Lymphoblastic Leukemia-Lymphoma · Phase 1
- Prostatic Neoplasms, Castration-Resistant · Phase 1/Phase 2
- Respiratory Tract Infections · Phase 3
Mechanism of action
- Serine/threonine-protein kinase mTORINHIBITOR
MTOR inhibitor
Dual MTOR/PIK3 inhibitor, ATP-competitive mTORC1/mTORC2 inhibitor
- PI3-kinase class IINHIBITOR
PI3-kinase class I inhibitor
Dual MTOR/PIK3 inhibitor, ATP-competitive mTORC1/mTORC2 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
Chemistry & pharmacology
Loading structure…
SMILES
Cn1c(=O)n(-c2ccc(C(C)(C)C#N)cc2)c2c3cc(-c4cnc5ccccc5c4)ccc3ncc21- Mol. weight
- 469.55 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaDactolisib ↗
- ChEMBLCHEMBL1879463 ↗
Also known as
- 2-methyl-2-(4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-1h-imidazo(4,5-c)quinolin-1-yl)phenyl)propanenitrile
- 2-methyl-2-(4-(3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo(4,5-c)quinolin-1-yl)phenyl)propanenitrile
- bez235
- bez235
- bez235
- bez-235
- bez-235
- dactolisib
- dactolisib
- dactolisib
- dactolisib
- dactolisib
- nvpbez235
- nvp bez235
- nvp-bez235
- nvp-bez235
- nvp-bez235
- nvp-bez235-nx
- nvp-bez235-nx
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04139915 | Phase 3 | Oct 21, 2019 | resTORbio, Inc. |
| NCT04668352 | Phase 3 | Apr 15, 2019 | P3 Research Ltd., resTORbio, Inc. |
| NCT03373903 | Phase 2 | Nov 15, 2017 | resTORbio, Inc. |
| NCT01856101 | Phase 2 | Feb 1, 2013 | Novartis, Université catholique de Louvain |
| NCT01717898 | Phase 1/Phase 2 (Phase 2) | Jan 1, 2013 | Novartis, University of California, San Francisco |
| NCT01658436 | Phase 2 | Nov 1, 2012 | Novartis |
| NCT01628913 | Phase 2 | Oct 1, 2012 | Novartis |
| NCT01634061 | Phase 1 | Sep 1, 2012 | Novartis |
| NCT01690871 | Phase 2 | Sep 1, 2012 | Novartis |
| NCT01756118 | Phase 1 | Jun 1, 2012 | J. W. Goethe University |
| NCT01290406 | Phase 2 | Mar 1, 2012 | Novartis |
| NCT01288092 | Phase 2 | Mar 1, 2012 | Novartis |
| NCT01471847 | Phase 1 | Feb 1, 2012 | Novartis |
| NCT01495247 | Phase 1/Phase 2 (Phase 2) | Jan 1, 2012 | Novartis |
| NCT01482156 | Phase 1 | Jan 1, 2012 | Novartis |
| NCT01508104 | Phase 1/Phase 2 (Phase 2) | Jan 1, 2012 | Novartis, University of Cincinnati |
| NCT01453595 | Phase 1/Phase 2 (Phase 2) | Oct 1, 2011 | Cornell University, Novartis |
| NCT01337765 | Phase 1 | Jul 1, 2011 | Array BioPharma |
| NCT01343498 | Phase 1 | Apr 1, 2011 | Novartis, SCRI Development Innovations |
| NCT01285466 | Phase 1 | Jan 1, 2011 | Novartis |
Showing 20 of 23 trials
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Organizations
Research & Development (11)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Novartis | For profit | 17 | 12 | 2 | 2006 |
| resTORbio, Inc. | For profit | 3 | 3 | 2 | 2017 |
| Array BioPharma | For profit | 1 | 1 | 1 | 2011 |
| Cornell University | Academic/Hospital | 1 | 1 | 1 | 2011 |
| J. W. Goethe University | Academic/Hospital | 1 | 1 | 1 | 2012 |
| P3 Research Ltd. | For profit | 1 | 0 | 1 | 2019 |
| SCRI Development Innovations | For profit | 1 | 1 | 1 | 2011 |
| Université catholique de Louvain | Academic/Hospital | 1 | 1 | 1 | 2013 |
| University of California, San Francisco | Academic/Hospital | 1 | 1 | 1 | 2013 |
| University of Cincinnati | Academic/Hospital | 1 | 1 | 1 | 2012 |
| Vanderbilt University | Academic/Hospital | 1 | 1 | 1 | 2010 |
11 organizations
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