Nereus (tradipitant)
Antiemetic Oral Capsule
Last reviewed · Source: First Databank (FDB) drug data
Overview
Tradipitant, a selective, high-affinity antagonist of human substance P/neurokinin-1 (NK1) receptors, is an antiemetic.
Tradipitant is a selective, high-affinity antagonist of human substance P/neurokinin-1 (NK1) receptors. The exact mechanism by which tradipitant exerts its antiemetic effect is not fully established; however, it is thought that substance P-mediated systems contribute to the nausea and vomiting in motion sickness. Tradipitant does not have substantial affinity for NK2, NK3, serotonin (5-HT3), dopamine (D2), cholinergic, or histamine (H1) receptors.
Tradipitant crosses the blood-brain barrier and occupies NK1 receptors in the brain, demonstrating a dose- and concentration-dependent increase in NK1 occupancy.
Following oral administration of tradipitant 85 mg and 170 mg in the fasting state, peak plasma concentrations are achieved at a median of 2 and 1.5 hours, respectively. Administration of tradipitant with a high-fat meal results in elevated peak plasma concentrations and a delayed time to peak plasma concentration. When tradipitant 85 mg was administered after a high-fat meal, peak plasma concentrations increased 4.7-fold and were delayed by 2 hours.
When tradipitant 170 mg was administered following a high-fat meal, peak plasma concentrations increased 6.9-fold and were delayed by 2.5 hours. Tradipitant is 96-99% bound to human plasma protein. Tradipitant is extensively metabolized, though mechanisms have not yet been fully characterized.
Metabolism has been proposed to occur via CYP3A4, CYP2C19, and CYP2C8 (to a lesser extent), and glucuronidation by UGT1A4 and UGT2B7; 4 major active metabolites (M2, M3, M4, and M8) are produced. Tradipitant is primarily excreted in the feces (80%), with minimal excretion in the urine (7%); unchanged drug was minimal in feces and not detected in urine. The mean elimination half-life is approximately 34 hours.
Mild to moderate renal impairment (eGFR >=30 mL/minute per 1.73 m2) does not have clinically important effects on the pharmacokinetics of tradipitant. The effect of severe renal impairment (eGFR <=29 mL/minute per 1.73 m2) or any degree of hepatic impairment (Child-Pugh Class A to C) on tradipitant pharmacokinetics is unknown.
USES: This medication is used to prevent vomiting caused by motion sickness. Tradipitant works by blocking one of the body's natural substances (substance P/neurokinin 1) that causes vomiting.
Generic name: tradipitant
Pronunciation: (tra-DI-pi-tant)
Drug class: Antiemetic
Therapeutic class: Gastrointestinal Therapy Agents
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
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Indications
The following indications are listed for Nereus:
- Prevention Of Motion Sickness
Also known as: Prevention Of Riders' Vertigo.
Dosing
No dosing information is available for this tab.
Administer tradipitant orally without food (>=1 hour prior to or 2 hours after a full meal), approximately 60 minutes before an event expected to cause vomiting induced by motion.
Store capsules at 25degreesC (excursions permitted to 15-30degreesC). Protect tradipitant capsules from exposure to light and moisture.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Nereus 85 Mg Capsule | Maintenance | Take 1 capsule (85 mg) by oral route once approximately 60 minutes before an event expected to cause vomiting induced by motion. |
No dosing information is available for this tab.
Drug interactions
In vitro studies suggest that tradipitant is a substrate of cytochrome P-450 (CYP) 3A4, CYP2C19, and, to a lesser extent, CYP2C8.
In vitro studies indicate that tradipitant may inhibit and induce CYP3A4; however, an in vivo study demonstrated no clinically significant pharmacokinetic differences when tradipitant and a CYP3A4 substrate were coadministered.
Tradipitant does not inhibit CYP1A2, 2B6, 2C8, 2C9, 2C19, or 2D6, and does not induce CYP1A2, 2B6, 2C8, 2C9, or 2C19.
Tradipitant is a substrate of P-glycoprotein (P-gp), UDP-glucuronosyltransferase (UGT) 1A4, and UGT2B7. Tradipitant is not a substrate of breast cancer resistance protein (BCRP), organic anion transporting polypeptide (OATP) 1B1, OATP1B3, multidrug and toxin extrusion protein (MATE) 1, or MATE2K.
In vitro studies indicate that tradipitant does not inhibit P-gp, BCRP, OATP1B1, OATP1B3, organic cation transporter 2 (OCT2), organic anion transporter (OAT) 1, OAT3, MATE1, or MATE2K.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*None.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
- No disease contraindications
Adverse reactions
The most common adverse reactions (incidence >=5%) reported with tradipitant in clinical studies were somnolence, headache, and fatigue.
There are no severe adverse reactions for this drug.
More Frequent
- Drowsy
Less Frequent
- Fatigue
- Headache disorder
Precautions
No enhanced messaging available.
Safety and efficacy of tradipitant have not been established in pediatric patients <18 years of age.
There are insufficient data on tradipitant use in pregnant women to inform a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes.
In animal studies, no adverse developmental effects were observed with oral tradipitant administration to pregnant rats during organogenesis through lactation, or to pregnant rabbits during organogenesis at doses up to approximately 3.3 and 1.4 times the exposure to tradipitant at the maximum recommended human dose (MRHD), respectively.
It is not known whether tradipitant is distributed into human milk. Effects of the drug on breastfed infants or milk production are also not known. Tradipitant is present in rat milk; therefore, it is likely to be present in human milk. Monitor breastfed infants for somnolence.
The manufacturer makes no specific dosage recommendations for geriatric patients (>=65 years of age).
In clinical studies, of tradipitant-treated patients, 69 (13%) were >=65 years of age and 4 (0.8%) were >=75 years of age. No overall differences in safety or efficacy were observed between geriatric patients (>=65 years of age) and younger adults (<65 years of age). No dosage adjustment based on age is required, but greater sensitivity of some older individuals cannot be ruled out.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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