Drugs / Dactolisib
Dactolisib
also known as
BEZ235 · RTB101 · Dactolisib tosilate · DACTOLISIB TOSYLATE · NSC-751249 · NVP-BEZ235 · NVP-BEZ235-ANA · NVP-BEZ235-NX
Small molecule targets MTOR via inhibition
Trials 26
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 111 trials | ||||||
| Phase 1 | NCT01634061 | Sep 2012 → Jul 2015 | castration-resistant prostate carcinoma | Novartis Pharmaceuticals | Completed | No outcome recorded |
| Phase 1 | NCT01756118 | Jun 2012 → Dec 2017 | acute lymphoblastic leukemia, acute myeloid leukemia, blast phase chronic myelogenous leukemia, BCR-ABL1 positive | Goethe University | Completed | No outcome recorded |
| Phase 1 | NCT01471847 | Feb → Jun 2012 | breast cancer | Novartis Pharmaceuticals | Completed | No outcome recorded |
| Phase 1 | NCT01482156 | Jan 2012 → Feb 2015 | breast cancer, renal cell carcinoma | Novartis Pharmaceuticals | Completed | No outcome recorded |
| Phase 1 | NCT01508104 | Jan 2012 → Feb 2014 | cancer | University of Cincinnati | Terminated | No outcome recorded Stop: Business |
| Phase 1 | NCT01337765 | Jul 2011 → Mar 2013 | cancer of unknown primary site | Pfizer | Completed | No outcome recorded |
| Phase 1 | NCT01343498 | Apr 2011 → Jan 2014 | cancer | SCRI Development Innovations, LLC | Completed | No outcome recorded |
| Phase 1 | NCT01285466 | Jan 2011 → Oct 2014 | cancer of unknown primary site | Novartis Pharmaceuticals | Completed | No outcome recorded |
| Phase 1 | NCT01248494 | Nov 2010 → Dec 2012 | breast cancer | Vanderbilt-Ingram Cancer Center | Completed | No outcome recorded |
| Phase 1 | NCT01195376 | Oct 2010 → Jul 2013 | neoplasm | Novartis Pharmaceuticals | Completed | No outcome recorded |
| Phase 1 | NCT00620594 | Dec 2006 → Jan 2013 | Cowden disease, breast cancer | Novartis Pharmaceuticals | Completed | No outcome recorded |
| Phase 1/24 trials | ||||||
| Phase 1/2 | NCT02430363 | Mar 2013 → Jan 2016 | glioblastoma | Medical Research Council | Unknown | No outcome recorded |
| Phase 1/2 | NCT01717898 | Jan → Sep 2013 | castration-resistant prostate carcinoma | Charles Ryan | Terminated | No outcome recorded |
| Phase 1/2 | NCT01495247 | Jan 2012 → May 2014 | female breast carcinoma | Novartis Pharmaceuticals | Terminated | No outcome recorded |
| Phase 1/2 | NCT01453595 | Oct 2011 → Apr 2014 | renal cell carcinoma | Memorial Sloan Kettering Cancer Center | Terminated | No outcome recorded |
| Phase 29 trials · 2 missed | ||||||
| Phase 2 | NCT04584710 | Oct 2020 → Feb 2021 overdue | COVID-19 | Restorbio Inc. | Active not recruiting | No outcome recorded |
| Phase 2 | NCT04409327 | Jul → Dec 2020 | COVID-19 | Restorbio Inc. | Terminated | No outcome recorded Stop: Enrollment |
| Phase 2 | NCT03373903 | Nov 2017 → May 2018 overdue | respiratory tract infectious disorder | Restorbio Inc. | Active not recruiting | Mixed |
| Phase 2 | NCT01856101 | Feb 2013 → Jan 2014 | transitional cell carcinoma | Cliniques universitaires Saint-Luc- Université Catholique de Louvain | Terminated | No outcome recorded |
| Phase 2 | NCT01658436 | Nov 2012 → Jul 2015 | pancreatic neuroendocrine tumor | Novartis Pharmaceuticals | Completed | Missed primary |
| Phase 2 | NCT01628913 | Oct 2012 → Sep 2014 | pancreatic neuroendocrine tumor | Novartis Pharmaceuticals | Terminated | Missed primary |
| Phase 2 | NCT01690871 | Sep 2012 → Jan 2015 | neoplasm with perivascular epithelioid cell differentiation | Novartis Pharmaceuticals | Withdrawn | No outcome recorded |
| Phase 2 | NCT01290406 | Mar 2012 → Sep 2014 | endometrial cancer | Novartis Pharmaceuticals | Withdrawn | No outcome recorded |
| Phase 2 | NCT01288092 | Mar 2012 → Sep 2015 | breast cancer | Novartis Pharmaceuticals | Withdrawn | No outcome recorded |
| Phase 32 trials | ||||||
| Phase 3 | NCT04139915 | Oct → Nov 2019 | respiratory tract infectious disorder | Restorbio Inc. | Withdrawn | No outcome recorded |
| Phase 3 | NCT04668352 | Apr → Dec 2019 | respiratory tract infectious disorder | Restorbio Inc. | Completed | No outcome recorded |
News releases announcing trial results or a regulatory action · 1
| Date | Issuer | Release |
|---|---|---|
| 2025-04-28 | Abbisko Therapeutics Co, Ltd | Results 2025 AACR | Abbisko Therapeutics Presents Late-Breaking Pre-clinical Research Results on ABSK112 (EGFR exon20ins), ABSK131 (PRMT5*MTA), and ABK-KRAS-1 (pan-KRAS) abbisko.com ↗
Combination therapies targeting glutamine metabolism (e.g., GLS1 inhibitors), MAPK (e.g., MEK inhibitors), and PI3K-AKT-mTOR pathways (e.g., BEZ235) reverse resistance and improve therapeutic efficacy in KEAP1-mutant cell lines. |
All press releases naming this drug 1 release
| Date | Issuer | Release |
|---|---|---|
| 2025-04-28 | Abbisko Therapeutics Co, Ltd | 2025 AACR | Abbisko Therapeutics Presents Late-Breaking Pre-clinical Research Results on ABSK112 (EGFR exon20ins), ABSK131 (PRMT5*MTA), and ABK-KRAS-1 (pan-KRAS) abbisko.com ↗ |
Evidence & citations 13 cited values
Every value below carries the sentence it was read from. 30 sources stand behind the page.
| Field | Value | Cited text |
|---|---|---|
| Known as | dactolisib | “The combination of everolimus and the imidazoquinoline derivative, BEZ235 (dactolisib), a dual PI3K/mTOR inhibitor, demonstrated synergy in a preclinical model.” PMID 28357727 ↗ Jun 2017 |
| Known as | BEZ235 | “Doses of oral BEZ235 (BID), supplied as 50mg, 200mg, 300mg or 400mg in SDS sachets, together with standard weekly paclitaxel at a fixed dose (80mg/m²) during 1h by i.v. in infusion.” NCT01495247 ↗21“BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor.” NCT02430363 ↗ |
| Known as | Dactolisib tosilate | ChEMBL registry synonym — accepted as the source's own label CHEMBL1879463 ↗ |
| Known as | DACTOLISIB TOSYLATE | ChEMBL registry synonym — accepted as the source's own label CHEMBL1879463 ↗ |
| Known as | NSC-751249 | ChEMBL registry synonym — accepted as the source's own label CHEMBL1879463 ↗ |
| Known as | NVP-BEZ235 | ChEMBL registry synonym — accepted as the source's own label CHEMBL1879463 ↗ |
| Known as | NVP-BEZ235-ANA | ChEMBL registry synonym — accepted as the source's own label CHEMBL1879463 ↗ |
| Known as | NVP-BEZ235-NX | ChEMBL registry synonym — accepted as the source's own label CHEMBL1879463 ↗ |
| Known as | RTB101 | “RTB101 (previously known as BEZ235), an oral mechanistic target of rapamycin (mTOR) inhibitor” PMID 33977284 ↗ May 2021 |
| Action | Inhibit | “an inhibitor of phosphatidylinositol 3'-kinase (PI3K)” NCT00620594 ↗ |
| Modality | Small molecule | “imidazoquinoline derivative” PMID 28357727 ↗ Jun 2017 |
| Route | Oral | “Patients receive oral BEZ235 once daily on days 1-28 of the first course.” NCT00620594 ↗ |
| Target | MTOR | “a potent inhibitor of both PI3K and mTOR” PMID 27286790 ↗ Jun 2016 |