Netupitant is a synthetic neurokinin-1 (NK1) receptor antagonist and pharmaceutical active pharmaceutical ingredient (API). It is an orally active antiemetic molecule that blocks the action of substance P at NK1 receptors.
Netupitant is used in combination with palonosetron hydrochloride in pharmaceutical formulations for the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV). PubChem and IUPHAR/BPS identify Netupitant as an approved NK1 receptor antagonist and antiemetic.
Netupitant is a specialized antiemetic pharmaceutical API relevant to oncology supportive care, chemotherapy-induced nausea and vomiting research, NK1 receptor antagonist development and pharmaceutical formulation.
The EMA assessment report confirms that the active-substance specification for Netupitant includes appearance, IR and HPLC identification, HPLC assay, HPLC impurities, residual solvents, water content, heavy metals, sulfated ash and particle-size distribution.
CAS Number: 290297-26-6
Molecular Formula: C₃₀H₃₂F₆N₄O
Molecular Weight: 578.59 g/mol
IUPAC Name: 2-[3,5-bis(trifluoromethyl)phenyl]-N,2-dimethyl-N-[4-(2-methylphenyl)-6-(4-methylpiperazin-1-yl)pyridin-3-yl]propanamide
Development Code: Ro 67-3189 / Ro-67-3189
Drug Class: Neurokinin-1 Receptor Antagonist
Therapeutic Class: Antiemetic
Therapeutic Area: Oncology Supportive Care / Gastroenterology
Molecule Type: Synthetic Small Molecule
Stereochemistry: Achiral
PubChem and FDA's Global Substance Registration System confirm the CAS number, molecular formula, molecular weight and achiral nature of Netupitant.
Netupitant is a selective NK1 receptor antagonist.
Its pharmacological activity includes:
Netupitant's NK1 receptor antagonism is particularly important in controlling the delayed phase of chemotherapy-induced emesis.
Netupitant API is relevant to:
Netupitant is used as part of an antiemetic combination with palonosetron, a 5-HT3 receptor antagonist.
The combination targets complementary pathways involved in chemotherapy-induced emesis and is used for prevention of acute and delayed nausea and vomiting associated with cancer chemotherapy.
The NK1 receptor is activated by substance P, a neuropeptide involved in the emetic response.
Netupitant selectively antagonizes NK1 receptors and therefore prevents substance-P-mediated signaling associated with chemotherapy-induced vomiting.
Netupitant is a synthetic organic compound with molecular formula C₃₀H₃₂F₆N₄O and molecular weight 578.59 g/mol. FDA's substance database classifies it as an achiral chemical substance with no defined stereocenters.
PubChem reports a calculated XLogP3-AA value of 6.8 and topological polar surface area of 39.7 Ų.
Published laboratory data describe Netupitant as a solid with a melting point around 160–161°C; however, this should not automatically be treated as an official pharmaceutical API release specification.
Netupitant is insoluble in water. A laboratory supplier's technical data reports solubility in ethanol and DMSO, while another analytical source reports slight solubility in chloroform, DMSO and methanol. These are useful physicochemical references but should not be confused with a pharmaceutical release specification.
A controlled Netupitant API manufacturing process may involve:
Typical Netupitant API testing may include:
The EMA assessment report specifically confirms that the Netupitant active-substance specification includes IR/HPLC identification, HPLC assay, HPLC impurities, residual solvents, water, heavy metals, sulfated ash and particle-size distribution.
Store Netupitant API in a tightly closed container under controlled pharmaceutical storage conditions, protected from excessive moisture, heat and direct light.
Final commercial storage conditions should be based on validated stability data and the applicable API specification.
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder or crystals |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | ≤ 1.5% |
| Water Content | NMT 1.0% |