Avacopan

Avacopan Uses, Dosage, Side Effects, Food Interaction and all others data.

Avacopan is under investigation in clinical trial NCT02994927 (A Phase 3 Clinical Trial of CCX168 (Avacopan) in Patients With ANCA-Associated Vasculitis).

Trade Name Avacopan
Availability Prescription only
Generic Avacopan
Avacopan Other Names Avacopan
Related Drugs azathioprine, rituximab, Rituxan, Truxima, Ruxience, Riabni, Tavneos
Type
Formula C33H35F4N3O2
Weight Average: 581.656
Monoisotopic: 581.266540031
Groups Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Avacopan
Avacopan

Food Interaction

[Moderate] ADJUST DOSING INTERVAL: Food significantly enhances the oral bioavailability of avacopan.

When a 30 mg capsule of avacopan was administered with a high-fat, high-calorie meal, avacopan peak plasma concentration (Cmax) and systemic exposure (AUC) increased by approximately 8% and 72%, respectively, while the time to reach peak concentration (Tmax) was delayed by approximately 4 hours (from 2.0 hours to 6.0 hours).



GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations of avacopan.

The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit.

Inhibition of hepatic CYP450 3A4 may also contribute.

The interaction has not been studied with grapefruit juice, but has been reported for itraconazole, a potent CYP450 3A4 inhibitor.

When avacopan was administered with itraconazole (200 mg once daily for 4 days), avacopan peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 87% and 119%, respectively.

In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands.

Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition.

Pharmacokinetic interactions involving grapefruit juice are also subject to a high degree of interpatient variability, thus the extent to which a given patient may be affected is difficult to predict.

Increased exposure to avacopan may increase the risk and
MANAGEMENT: To ensure maximal oral absorption, avacopan should be administered with food.

Patients should preferably avoid or limit consumption of grapefruit, grapefruit juice, or any supplement containing grapefruit extract during avacopan therapy.

Innovators Monograph

You find simplified version here Avacopan

*** Taking medicines without doctor's advice can cause long-term problems.
Share