Action and Spectrum

Actions and Spectrum 

rolapitant functions by inhibiting substance P, a neurotransmitter implicated in causing nausea and vomiting. The prevention of delayed chemotherapy-induced nausea and vomiting (CINV) is the only indication for the use of rolapitant. It works well against CINV in both the acute and delayed phases.  

Drug Interaction

Adverse Reaction

Frequency defined  

1-10% 

Neutropenia (9%)  

Dyspepsia (4%) 

Urinary tract infection (4%) 

Decreased appetite (9%) 

Dizziness (6%)  

Anemia (3%) 

Stomatitis (4%)  

Hiccups (5%) 

Neutropenia (7%) 

Abdominal pain (3%)  

Black Box Warning

Black Box Warning 

None

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• rolapitant should not be used in individuals with a known hypersensitivity or allergic reaction to rolapitant or any of its components. 

Caution: 

• rolapitant should not be administered to people who need to take strong CYP3A4 inducers on a regular basis. 

Pregnancy / Lactation

Pregnancy consideration:     

Pregnancy category: N/A 

Lactation: Excretion into human milk is unknown  

Pregnancy Categories:         

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.  

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women. 

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 

Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology  

rolapitant works by attaching to and inhibiting the NK1 receptor in the vomiting center of the central nervous system. It blocks the signaling process by preventing substance P from interacting with the NK1 receptor.  

Pharmacodynamics 

rolapitant is used in combination with other antiemetic medications, such as 5-HT3 receptor antagonist and a corticosteroid. This combination therapy targets multiple pathways involved in the emetic process, including serotonin receptors and corticosteroid receptors. 

Pharmacokinetics 

Absorption   

rolapitant is absorbed when taken orally. It is rapidly absorbed from the gastrointestinal track.  

Distribution 

The drug has a large volume of distribution throughout the body. 

Metabolism 

rolapitant undergoes extensive metabolism in the liver. 

Elimination and excretion 

The elimination of rolapitant and its metabolites occurs through feces. 

Adminstartion

Administration 

rolapitant is available as an oral tablet for administration.

Patient Information Leaflet

Patient information leaflet 

Generic Name: rolapitant 

Why do we use rolapitant? 

rolapitant is used as an antiemetic drug for the prevention of chemotherapy-induced nausea and vomiting (CINV).