fosnetupitant
Trade name: Akynzeo
Approved
Apr 19, 2018
Fosnetupitant is a prodrug form of netupitant. Netupitant is a selective antagonist of human substance P/neurokinin 1 (NK-1) receptors. Upon intravenous administration, fosnetupitant is converted by phosphatases to its active form. It competitively binds to and blocks the activity of NK-1 receptors in the central nervous system, by inhibiting binding of substance P (SP) to NK-1 receptors. This prevents delayed emesis, which is associated with SP secretion. AKYNZEO® is a combination of palonosetron, a serotonin-3 receptor antagonist, and netupitant (capsules for oral use) or fosnetupitant (injections for intravenous use). AKYNZEO® for injection is indicated in combination with dexamethasone in adults for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. — NCATS
Clinical trial activity
2 trials · 4 clinical orgs · 1 marketing orgs
Earliest trial started Mar 16, 2018 (NCT03403712)
Timeline
Indications
Mechanism of action
- Neurokinin 1 receptorANTAGONIST
Neurokinin 1 receptor antagonist
Inhibits substance P mediated activation of NK1 receptors, activation is linked to delayed emesis.
Approval history
- approvedApr 19, 2018
Chemistry & pharmacology
SMILES
CN(C(=O)C(C)(C)C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)C2=C(C=C(N=C2)N3CC[N+](C)(COP(O)([O-])=O)CC3)C4=C(C)C=CC=C4- Mol. weight
- 688.5976 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Parenteral
- Availability
- Prescription Only
Oral
No
Parenteral
Yes
Topical
No
Sources
- WikipediaNetupitant/palonosetron ↗
- NCATST672P80L2S ↗
- ChEMBLCHEMBL3989919 ↗
- ChEMBLCHEMBL3989917 ↗
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06840769 | Phase 1 | Jun 17, 2023 | Cross Research S.A., Helsinn |
| NCT03403712 | Phase 3 | Mar 16, 2018 | George Clinical Pty Ltd, Helsinn, PSI CRO |
Organizations
Research & Development (4)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Helsinn | For profit | 2 | 2 | 2 | 2018 |
| Cross Research S.A. | For profit | 1 | 0 | 1 | 2023 |
| George Clinical Pty Ltd | Academic/Hospital | 1 | 0 | 1 | 2018 |
| PSI CRO | For profit | 1 | 0 | 1 | 2018 |