fosnetupitant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| neurokinin NK1 (substance P) receptor antagonist | 5283 | 1703748-89-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Netupitant is a selective antagonist of human substance P/neurokinin 1 (NK-1) receptors. Delayed emesis has been largely associated with the activation of tachykinin family neurokinin 1 (NK-1) receptors (broadly distributed in the central and peripheral nervous systems) by substance P. As shown in in vitro and in vivo studies, netupitant inhibits substance P mediated responses.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 1.40 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 19, 2018 | FDA | HELSINN HLTHCARE | |
| March 28, 2022 | PMDA | Taiho Pharmaceutical Co., Ltd. |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
None
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chemotherapy-induced nausea and vomiting | indication | 236084000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.75 | acidic |
| pKa2 | 3.93 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML) | AKYNZEO | HELSINN HLTHCARE | N210493 | May 27, 2020 | RX | SOLUTION | INTRAVENOUS | 9186357 | Nov. 18, 2030 | USE 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 |
| EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL | AKYNZEO | HELSINN HLTHCARE | N210493 | April 19, 2018 | RX | POWDER | INTRAVENOUS | 9186357 | Nov. 18, 2030 | USE 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 |
| EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML) | AKYNZEO | HELSINN HLTHCARE | N210493 | May 27, 2020 | RX | SOLUTION | INTRAVENOUS | 10828297 | Dec. 17, 2030 | USE 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 |
| EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL | AKYNZEO | HELSINN HLTHCARE | N210493 | April 19, 2018 | RX | POWDER | INTRAVENOUS | 10828297 | Dec. 17, 2030 | USE 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 |
| EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML) | AKYNZEO | HELSINN HLTHCARE | N210493 | May 27, 2020 | RX | SOLUTION | INTRAVENOUS | 10208073 | May 23, 2032 | USE 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 |
| EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML) | AKYNZEO | HELSINN HLTHCARE | N210493 | May 27, 2020 | RX | SOLUTION | INTRAVENOUS | 8895586 | May 23, 2032 | USE 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 |
| EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML) | AKYNZEO | HELSINN HLTHCARE | N210493 | May 27, 2020 | RX | SOLUTION | INTRAVENOUS | 9403772 | May 23, 2032 | USE 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 |
| EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL | AKYNZEO | HELSINN HLTHCARE | N210493 | April 19, 2018 | RX | POWDER | INTRAVENOUS | 10208073 | May 23, 2032 | USE 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 |
| EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL | AKYNZEO | HELSINN HLTHCARE | N210493 | April 19, 2018 | RX | POWDER | INTRAVENOUS | 8895586 | May 23, 2032 | USE 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 |
| EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL | AKYNZEO | HELSINN HLTHCARE | N210493 | April 19, 2018 | RX | POWDER | INTRAVENOUS | 9403772 | May 23, 2032 | USE 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 |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML) | AKYNZEO | HELSINN HLTHCARE | N210493 | May 27, 2020 | RX | SOLUTION | INTRAVENOUS | April 19, 2023 | NEW CHEMICAL ENTITY |
| EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL | AKYNZEO | HELSINN HLTHCARE | N210493 | April 19, 2018 | RX | POWDER | INTRAVENOUS | April 19, 2023 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Substance-P receptor | GPCR | ANTAGONIST | Ki | 9.02 | SCIENTIFIC LITERATURE | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| T672P80L2S | UNII |
| C4691680 | UMLSCUI |
| CHEMBL3989917 | ChEMBL_ID |
| 71544786 | PUBCHEM_CID |
| DB14019 | DRUGBANK_ID |
| CHEMBL3989919 | ChEMBL_ID |
| D11065 | KEGG_DRUG |
| 10146 | INN_ID |
| 34267 | MMSL |
| d08869 | MMSL |
| 017511 | NDDF |
| 017512 | NDDF |
| 781258008 | SNOMEDCT_US |
| 4037545 | VANDF |
| 1643757-72-5 | SECONDARY_CAS_RN |
| 2044416 | RXNORM |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| AKYNZEO | HUMAN PRESCRIPTION DRUG LABEL | 2 | 69639-102 | INJECTION | 260 mg | INTRAVENOUS | NDA | 26 sections |
| AKYNZEO | HUMAN PRESCRIPTION DRUG LABEL | 2 | 69639-102 | INJECTION | 260 mg | INTRAVENOUS | NDA | 26 sections |
| AKYNZEO | HUMAN PRESCRIPTION DRUG LABEL | 2 | 69639-102 | INJECTION | 260 mg | INTRAVENOUS | NDA | 26 sections |
| AKYNZEO | HUMAN PRESCRIPTION DRUG LABEL | 2 | 69639-105 | INJECTION | 260 mg | INTRAVENOUS | NDA | 26 sections |
| AKYNZEO | HUMAN PRESCRIPTION DRUG LABEL | 2 | 69639-105 | INJECTION | 260 mg | INTRAVENOUS | NDA | 26 sections |
| AKYNZEO | HUMAN PRESCRIPTION DRUG LABEL | 2 | 69639-105 | INJECTION | 260 mg | INTRAVENOUS | NDA | 26 sections |
| AKYNZEO | HUMAN PRESCRIPTION DRUG LABEL | 2 | 69639-106 | INJECTION | 260 mg | INTRAVENOUS | NDA | 26 sections |