rolapitant
Trade name: varubi
Approved
Sep 1, 2015
Rolapitant (VARUBI) is neurokinin 1 (NK1) receptor antagonist. Rolapitant does not have significant affinity for the NK2 or NK3 receptors. Drug is indicated in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy. Most common adverse reactions are: neutropenia and hiccups at Cisplatin Based Highly Emetogenic Chemotherapy; decreased appetite, neutropenia and dizziness at Moderately Emetogenic Chemotherapy and Combinations of Anthracycline and Cyclophosphamide. Inhibition of BCRP and P-gp by rolapitant can increase plasma concentrations of the concomitant drug and potential for adverse reactions. Strong CYP3A4 Inducers (e.g., rifampin) can significantly reduce plasma concentrations of rolapitant and decrease the efficacy of VARUBI. — NCATS
Clinical trial activity
12 trials · 7 clinical orgs · 2 marketing orgs
Earliest trial started Sep 1, 2006 (NCT00394966)
Timeline
2000s
2010s
- Jan 1, 2012
- Jan 1, 2014
- Sep 1, 2015
Tesaro — Earliest FDA Approval
- Sep 1, 2015
Tersera Theraps Llc — NDA Secondary Org
- Sep 1, 2015
Tesaro — NDA Organization
- Sep 1, 2015
Tersera Theraps Llc — Marketing Organization
Indications
Approved for
Mechanism of action
- Neurokinin 1 receptorANTAGONIST
TACR1 antagonist
Approval history
- approvedSep 1, 2015
Chemistry & pharmacology
SMILES
C[C@@H](OC[C@@]1(c2ccccc2)CC[C@]2(CCC(=O)N2)CN1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1- Mol. weight
- 500.48 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral, Parenteral
- Availability
- Prescription Only
Oral
Yes
Parenteral
Yes
Topical
No
Sources
- ChEMBLCHEMBL3707331 ↗
- WikipediaRolapitant ↗
- NCATSNLE429IZUC ↗
- ChEMBLCHEMBL3707330 ↗
Also known as
- 8-((1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1,7-diazaspiro(4,5)decan-2-one
- rolapitant
- rolapitant
- rolapitant
- rolapitant
- rolapitant
- rolapitant
- rolapitant
- rolapitant
- rolapitant
- rolapitant
- rolapitant
- rolapitant hcl
- rolapitant hcl
- rolapitant hydrochloride
- rolapitant hydrochloride
- rolapitant hydrochloride
- rolapitant hydrochloride
- sch619734
- sch 619734
- sch 619734
- sch 619734
- sch 619734
- sch-619734
- sch-619734
- varubi
- varubi
- varubi
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03960151 | Phase 2 | May 31, 2018 | Hoosier Cancer Research Network, Indiana University, Tesaro |
| NCT02991456 | Phase 2 | Jun 15, 2017 | Duke University, Tesaro |
| NCT02732015 | Phase 2 | Oct 1, 2016 | Tesaro, University of Texas at Houston |
| NCT02434861 | Phase 1 | May 1, 2015 | Tesaro |
| NCT02382666 | Phase 1 | Jan 1, 2015 | Tesaro |
| NCT02285647 | Phase 1 | Sep 1, 2014 | Tesaro |
| NCT01500226 | Phase 3 | Feb 1, 2012 | Tesaro |
| NCT01500213 | Phase 3 | Feb 1, 2012 | Tesaro |
| NCT01499849 | Phase 3 | Feb 1, 2012 | Tesaro |
| NCT00539721 | Phase 2 | Oct 1, 2007 | Merck |
| NCT00506545 | Phase 2 | Jan 1, 2007 | Merck |
| NCT00394966 | Phase 2 | Sep 1, 2006 | Schering-Plough |
Organizations
Research & Development (7)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Tesaro | For profit | 9 | 6 | 3 | 2012 |
| Merck | For profit | 2 | 2 | 1 | 2007 |
| Duke University | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Hoosier Cancer Research Network | Academic/Hospital | 1 | 1 | 1 | 2018 |
| Indiana University | Academic/Hospital | 1 | 0 | 1 | 2018 |
| Schering-Plough | For profit | 1 | 1 | 1 | 2006 |
| University of Texas at Houston | Academic/Hospital | 1 | 1 | 1 | 2016 |
Marketing (4)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Tersera Theraps Llc | For profit | NDA2 | Sep 1, 2015 |
| Tersera Theraps Llc | For profit | MKTG | Sep 1, 2015 |
| Tesaro | For profit | NDA | Sep 1, 2015 |
| Tesaro | For profit | IND | Oct 6, 2005 |