Name: | aprepitant |
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PubChem Compound ID: | 11214788 |
Molecular formula: | C23H21F7N4O3 |
Molecular weight: | 536.419 g/mol |
Name: | aprepitant |
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Name (isomeric): | DB00673 |
Drug Type: | small molecule |
Synonyms: |
MK-0517; MK-869
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Brand: | Emend |
Category: | Antiemetics |
CAS number: | 170729-80-3 |
Indication: | For the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy, including high-dose cisplatin (in combination with other antiemetic agents). |
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Pharmacology: |
Aprepitant, an antiemetic, is 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 hum...
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Mechanism 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 Aprepit...
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Absorption: | The mean absolute oral bioavailability of aprepitant is approximately 60 to 65%. |
Protein binding: | >95% |
Biotransformation: | 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. |
Route of elimination: | Aprepitant is eliminated primarily by metabolism; aprepitant is not renally excreted. Aprepitant is excreted in the milk of rats. It is not known whether this drug is excreted in human milk. |
Half Life: | 9-13 hours |
Clearance: | Apparent plasma cl=62-90 mL/min |
Affected organisms: | Humans and other mammals |
Food interaction: |
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Drug interaction: |
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Name: | aprepitant |
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Name (isomeric): | DB06717 |
Drug Type: | small molecule |
Brand: | Emend® IV |
Category: | Antiemetics |
CAS number: | 172673-20-0 |
Indication: | For the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy. |
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Pharmacology: |
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....
show more » |
Mechanism 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 Aprepit...
show more » |
Protein binding: | 95% + |
Biotransformation: | 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. |
Route of elimination: | Aprepitant is eliminated primarily by metabolism; aprepitant is not renally excreted. Aprepitant is excreted in the milk of rats. It is not known whether this drug is excreted in human milk. |
Half Life: | 9-13 hours |
Drug interaction: |
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