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US Approved Rx

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Primary Target

Neurokinin 1 receptor

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Neurokinin 2 receptor

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Neurokinin 3 receptor

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Approved

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Approval Year

2015

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Condition

Delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy

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Treatment Modality

Secondary

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CNS Penetrant

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Schering-Plough

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ATC Level 4

Other antiemetics

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ROLAPITANT

NLE429IZUC

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Status:

US Approved Rx (2015)

First approved in 2015

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Neurokinin 3 receptor

Neurokinin 2 receptor

Neurokinin 1 receptor

Conditions:

Delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy

Rolapitant (VARUBI) is neurokinin 1 (NK1) receptor antagonist. Rolapitant does not have significant affinity for the NK2 or NK3 receptors. Drug is indicated in combination with other antiemetic agents in adults for the prevention of delayed nausea an...

d vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy. Most common adverse reactions are: neutropenia and hiccups at Cisplatin Based Highly Emetogenic Chemotherapy; decreased appetite, neutropenia and dizziness at Moderately Emetogenic Chemotherapy and Combinations of Anthracycline and Cyclophosphamide. Inhibition of BCRP and P-gp by rolapitant can increase plasma concentrations of the concomitant drug and potential for adverse reactions. Strong CYP3A4 Inducers (e.g., rifampin) can significantly reduce plasma concentrations of rolapitant and decrease the efficacy of VARUBI.

ROLAPITANT HYDROCHLORIDE ANHYDROUS

J7Z9DBN8J0

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Status:

US Approved Rx (2015)

First approved in 2015

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Neurokinin 3 receptor

Neurokinin 2 receptor

Neurokinin 1 receptor

Conditions:

Delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy

Rolapitant (VARUBI) is neurokinin 1 (NK1) receptor antagonist. Rolapitant does not have significant affinity for the NK2 or NK3 receptors. Drug is indicated in combination with other antiemetic agents in adults for the prevention of delayed nausea an...

d vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy. Most common adverse reactions are: neutropenia and hiccups at Cisplatin Based Highly Emetogenic Chemotherapy; decreased appetite, neutropenia and dizziness at Moderately Emetogenic Chemotherapy and Combinations of Anthracycline and Cyclophosphamide. Inhibition of BCRP and P-gp by rolapitant can increase plasma concentrations of the concomitant drug and potential for adverse reactions. Strong CYP3A4 Inducers (e.g., rifampin) can significantly reduce plasma concentrations of rolapitant and decrease the efficacy of VARUBI.

ROLAPITANT HYDROCHLORIDE

57O5S1QSAQ

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Search for Structure

Status:

US Approved Rx (2015)

First approved in 2015

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Neurokinin 3 receptor

Neurokinin 2 receptor

Neurokinin 1 receptor

Conditions:

Delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy

Rolapitant (VARUBI) is neurokinin 1 (NK1) receptor antagonist. Rolapitant does not have significant affinity for the NK2 or NK3 receptors. Drug is indicated in combination with other antiemetic agents in adults for the prevention of delayed nausea an...

d vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy. Most common adverse reactions are: neutropenia and hiccups at Cisplatin Based Highly Emetogenic Chemotherapy; decreased appetite, neutropenia and dizziness at Moderately Emetogenic Chemotherapy and Combinations of Anthracycline and Cyclophosphamide. Inhibition of BCRP and P-gp by rolapitant can increase plasma concentrations of the concomitant drug and potential for adverse reactions. Strong CYP3A4 Inducers (e.g., rifampin) can significantly reduce plasma concentrations of rolapitant and decrease the efficacy of VARUBI.

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