netupitant
Trade name: Akynzeo
Small moleculeapproved
Approved
Oct 10, 2014
Netupitant is an antiemitic drug approved by the FDA in October 2014 for use in combination with palonosetron for the prevention of acute and delayed vomiting and nausea associated with cancer chemotherapy including highly emetogenic chemotherapy. — NCATS
Clinical trial activity
24 trials · 33 clinical orgs · 1 marketing orgs
Phase 1
1
Phase 2
16
Phase 3
9
Phase 4
4
Earliest trial started Apr 1, 2011 (NCT01339260)
Timeline
Indications
Approved for
Studied for
- Breast Neoplasms · Phase 3
- Drug-Related Side Effects and Adverse Reactions · Phase 4
- Drug Therapy · Phase 3
- Endometrial Neoplasms · Phase 4
- Gallbladder Neoplasms · Phase 2
- Healthy Volunteers · Phase 1
- Nausea · Phase 2/Phase 3
- Neoplasms · Phase 4
- Reperfusion Injury · Phase 2
- Uterine Cervical Neoplasms · Phase 2/Phase 3
- Vomiting · Phase 2/Phase 3
Mechanism of action
- Neurokinin 1 receptorANTAGONIST
TACR1 antagonist
Combination products
akynzeo
with palonosetron
Also known as nepa (300mg netupitant/0.5mg palonosetron)
Approval history
- approvedOct 10, 2014
Chemistry & pharmacology
Loading structure…
SMILES
CN(C(=O)C(C)(C)C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)C2=CN=C(C=C2C3=C(C)C=CC=C3)N4CCN(C)CC4- Mol. weight
- 578.5917 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaNetupitant ↗
- NCATS7732P08TIR ↗
- ChEMBLCHEMBL206253 ↗
Also known as
- 2-[3,5-bis(trifluoromethyl)phenyl]-n,2-dimethyl-n-[4-(2-methylphenyl)-6-(4-methyl-1-piperazinyl)-3-pyridinyl]propanamide
- 2-[3,5-bis(trifluoromethyl)phenyl]-n,2-dimethyl-n-[4-(2-methylphenyl)-6-(4-methyl-1-piperazinyl)-3-pyridinyl]propanamide
- akynzeo
- akynzeo
- akynzeo
- netupitant
- netupitant
- netupitant
- netupitant
- netupitant
- netupitant
- netupitant
- netupitant
- netupitant / palonosetron
- netupitant / palonosetron hydrochloride
- netupitant - palosentron
- netupitant, palosentron drug combination
- pro-netupitant
- ro 67-3189/000
- ro 67-3189/000
- ro 67-3189/000
- ro 67-3189/000
- ro 67-3189/000
- ro-673189000
- ro-673189000
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07254416 | Phase 4 | Dec 15, 2025 | Henan Medical University, Jiao Tong University, Shaanxi Provincial People's Hospital, Shanxi Bethune Hospital, Tianjin Medical University |
| NCT06331520 | Phase 3 | May 1, 2024 | Fudan University |
| NCT06726291 | Phase 4 | Feb 26, 2024 | University of Milan |
| NCT06102447 | N/A | Nov 1, 2023 | University of Electronic Science and Technology of China |
| NCT06065722 | Phase 2 | Sep 9, 2023 | Helsinn, Simon Williamson Clinic |
| NCT04817189 | Phase 4 | Feb 1, 2021 | Helsinn, The Hong Kong Polytechnic University |
| NCT04388761 | Phase 2 | Feb 1, 2021 | Mayo Clinic |
| NCT04486157 | Phase 1 | Jan 31, 2021 | Catholic University of Korea, Inno.N |
| NCT04669132 | Phase 2 | Dec 17, 2020 | Instituto Brasileiro de Controle do Cancer |
| NCT04362449 | Phase 2 | Jan 2, 2019 | Chugai, University of London |
| NCT03831633 | Phase 4 | Sep 19, 2018 | Vifor Inc. |
| NCT03668639 | Phase 2/Phase 3 (Phase 3) | Sep 5, 2018 | Helsinn, University of Southern Denmark |
| NCT03403712 | Phase 3 | Mar 16, 2018 | George Clinical Pty Ltd, Helsinn, PSI CRO |
| NCT03367572 | Phase 3 | Mar 9, 2018 | National Cancer Institute (NCI), University of Rochester |
| NCT03386617 | Phase 2 | Feb 27, 2018 | Chinese University of Hong Kong, University of Toronto |
| NCT03204279 | Phase 2 | Aug 31, 2017 | Helsinn |
| NCT03040726 | Phase 2/Phase 3 (Phase 3) | May 3, 2017 | Helsinn, University of Texas at Houston |
| NCT03097588 | Phase 2 | May 1, 2017 | National Cancer Institute (NCI), Oregon Health and Science University |
| NCT03008213 | Phase 2 | Jan 1, 2017 | University of California, San Diego |
| NCT04201769 | Phase 3 | Nov 25, 2016 | Hospital Agostino Gemelli, Istituto Nazionale per lo Studio e la Cura dei Tumori, Oncotech |
Showing 20 of 24 trials
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Organizations
Research & Development (33)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Helsinn | For profit | 9 | 6 | 3 | 2011 |
| National Cancer Institute (NCI) | Government | 2 | 0 | 2 | 2017 |
| Oncotech | For profit | 2 | 2 | 2 | 2016 |
| Parexel | For profit | 2 | 0 | 1 | 2011 |
| PSI CRO | For profit | 2 | 0 | 1 | 2015 |
| Catholic University of Korea | Academic/Hospital | 1 | 0 | 1 | 2021 |
| Chinese University of Hong Kong | Academic/Hospital | 1 | 1 | 1 | 2018 |
| Chugai | For profit | 1 | 0 | 1 | 2019 |
| Fondazione Giovanni Pascale | Academic/Hospital | 1 | 0 | 1 | 2016 |
| Fudan University | Academic/Hospital | 1 | 1 | 1 | 2024 |
| George Clinical Pty Ltd | Academic/Hospital | 1 | 0 | 1 | 2018 |
| Henan Medical University | Academic/Hospital | 1 | 0 | 1 | 2025 |
| Hospital Agostino Gemelli | Academic/Hospital | 1 | 0 | 1 | 2016 |
| Inno.N | For profit | 1 | 1 | 1 | 2021 |
| Instituto Brasileiro de Controle do Cancer | Academic/Hospital | 1 | 1 | 1 | 2020 |
| Istituto Nazionale per lo Studio e la Cura dei Tumori | Academic/Hospital | 1 | 0 | 1 | 2016 |
| Jiao Tong University | Academic/Hospital | 1 | 0 | 1 | 2025 |
| Mayo Clinic | Academic/Hospital | 1 | 1 | 1 | 2021 |
| Oregon Health and Science University | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Shaanxi Provincial People's Hospital | Academic/Hospital | 1 | 0 | 1 | 2025 |
33 organizations
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