Fosrolapitant is a neurokinin-1 (NK1) receptor antagonist developed as a prodrug of rolapitant. It is designed to undergo conversion to rolapitant, the active NK1 receptor antagonist. Fosrolapitant has been investigated for its potential use in the prevention of chemotherapy-induced nausea and vomiting (CINV).
Fosrolapitant is a specialized pharmaceutical research compound associated with antiemetic drug development. Its prodrug design is intended to provide an alternative route for delivering the active NK1 receptor antagonist rolapitant.
CAS Number: 1398335-28-8
Molecular Formula: C30H28F6N4O5
Molecular Weight: 638.57 g/mol
Drug Class: Antiemetic / NK1 Receptor Antagonist Prodrug
Active Metabolite: Rolapitant
Therapeutic Area: Oncology Supportive Care
Fosrolapitant is designed to be converted to rolapitant, which selectively antagonizes neurokinin-1 receptors. NK1 receptors are activated by substance P and are involved in the vomiting reflex. Blocking these receptors can help inhibit pathways associated with chemotherapy-induced nausea and vomiting.
Fosrolapitant has been investigated as a prodrug approach for delivering rolapitant for the prevention of chemotherapy-induced nausea and vomiting. NK1 receptor antagonism is particularly relevant to the delayed phase of CINV.
Fosrolapitant is the prodrug, while rolapitant is the pharmacologically active NK1 receptor antagonist. The conversion of fosrolapitant to rolapitant provides the active compound responsible for NK1 receptor blockade.
Fosrolapitant is a fluorinated, phosphate-containing prodrug associated with a relatively high molecular weight. Its molecular formula is C30H28F6N4O5 and its molecular weight is 638.57 g/mol.
Fosrolapitant API quality assessment may include identity testing by IR and LC-MS, HPLC assay, related-substance analysis, water content, residual solvents, elemental impurity testing and other analytical tests appropriate for pharmaceutical research and development.
Fosrolapitant should be stored in a tightly closed container under controlled laboratory conditions and protected from excessive heat, moisture and direct light. Storage conditions should follow the applicable stability data and material-specific specification.
Fosrolapitant is relevant to pharmaceutical research involving NK1 receptor antagonism and antiemetic drug development. Its prodrug approach has been investigated as a means of delivering rolapitant for supportive care in oncology.
Fosrolapitant is a prodrug of the NK1 receptor antagonist rolapitant and has been investigated for applications in the prevention of chemotherapy-induced nausea and vomiting. It is identified by CAS Number 1398335-28-8, with molecular formula C30H28F6N4O5 and molecular weight 638.57 g/mol.
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 2.0% |
| Heavy Metals | NMT 20 ppm |
| Individual Impurity | ≤ 0.5% |
| Water Content | NMT 2.0% |