Placeholder

Fosaprepitant Dimeglumine

  • # LGM Pharma is a Fosaprepitant Dimeglumine CAS# 265121-04-8 API supplier distributor based in the USA. Inquire about DMF, cGMP, price, availability, samples, sourcing, purity and more.
  • # Questions? Call our customer API support number 1-(800)-881-8210.
  • # LGM Pharma offers this active ingredient but not the finished dosage forms.
  • Inquire about this product >>

Product Details:

  • Product Name: Fosaprepitant Dimeglumine
  • CAS #: 265121-04-8
  • Mode of Action:

    Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with Aprepitant have shown that it crosses the blood brain barrier and occupies brain NK1 receptors. Animal and human studies show that Aprepitant augments the antiemetic activity of the 5-HT3-receptor antagonist ondansetron and the corticosteroid ethasone and inhibits both the acute and delayed phases of cisplatin induced emesis. In summary, the active form of fosaprepitant is as an NK1 antagonist which is because it blocks signals given off by NK1 receptors. This therefore decreases the likelihood of vomiting in patients experiencing.

  • Pharmacodynamics:

    Fosaprepitant is a prodrug of Aprepitant. Once biologically activated, the drug acts as a substance P/neurokinin 1 (NK1) receptor antagonist which, in combination with other antiemetic agents, is indicated for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CI NV).

  • Metabolism:

    Aprepitant is metabolized primarily by CYP3A4 with minor metabolism by CYP1A2 and CYP2C19. Seven metabolites of aprepitant, which are only weakly active, have been identified in human plasma.

  • DrugBank: DB06717
  • Formula: C23-H22-F7-N4-O6-P.2C7-H17-N-O5
  • Molecular Mass: 1004.8354
  • Synonyms: Emend, Fosaprepitant dimeglumine, Ivemend, MK-0517, UNII-D35FM8T64X
  • SMILES: C[C@H](c1cc(cc(c1)C(F)(F)F)C(F)(F)F)O[C@@H]2[C@@H](N(CCO2)Cc3[nH]c(=O)n(n3)P(=O)(O)O)c4ccc(cc4)F.CNC[C@@H]([C@H]([C@@H]([C@@H](CO)O)O)O)O.CNC[C@@H]([C@H]([C@@H]([C@@H](CO)O)O)O)O
  • AHFS Code: 56:22.9
Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

API’s From Quality Manufacturers:

  • Streamlined API supply towards initial research stages as well as larger quantities of cGMP material for clinical trials and product commercialization
  • Premium quality GMP certified and fully accredited API manufacturing plants

 

  • Technical packages as well as access to filed DMF,
    ASMF or CEP (subject to availability)
  • Regulatory and technical assistance towards any
    submission type based on specific customer requirements