Ixazomib

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

Ixazomib a second generation proteasome inhibitor (PI) and the first oral PI approved by the FDA in November 2015 for multiple myeloma treatment in combination with 2 other therapies (lenalidomide and dexamethasone) for patients who have received at least 1 prior therapy. It was found to have similar efficacy to bortezomib (the first PI approved for multiple myeloma therapy) in the control of myeloma growth and prevention of bone loss. Ixazomib citrate is marketed by Takeda Pharmaceuticals under the brand name Ninlaro, which is a prodrug that becomes quickly converted to its active metabolite, ixazomib, after administration.

In vitro studies have shown ixazomib to induce apoptosis in multiple myeloma cells sensitive or resistant to other conventional therapies. In mouse xenograft models, ixazomib induced tumor growth inhibition.

Ixazomib
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Ixazomib
Availability	Prescription only
Generic	Ixazomib
Ixazomib Other Names	Ixazomib
Related Drugs	Revlimid, Velcade, Darzalex, Pomalyst, Ninlaro, Kyprolis
Weight	2.3mg, 3mg, 4mg
Type	Oral capsule
Formula	C₁₄H₁₉BCl₂N₂O₄
Weight	Average: 361.03 Monoisotopic: 360.081492
Protein binding	99%
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Ixazomib is a monoclonal antibody used with other medications to treat multiple myeloma in patients who have received one other therapy already.

Ixazomib is indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received at least one prior therapy.

Ixazomib is also used to associated treatment for these conditions: Multiple Myeloma (MM)

How Ixazomib works

Ixazomib is an N-capped dipeptidyl leucine boronic acid which reversibly inhibits the CT-L proteolytic (β5) site of the 20S proteasome. At higher concentrations, ixazomib also seems to inhibit the proteolytic β1 and β2 subunits and to induce accumulation of ubiquitinated proteins.

Toxicity

Drug-induced liver injury, hepatocellular injury, hepatic steatosis, hepatitis cholestatic and hepatotoxicity have each been reported in <1% of patients. Ixazomib can cause fetal harm when administered to pregnant women, and therefore it should also be advised to women of reproductive age to avoid becoming pregnant on ixazomib.

Food Interaction

Avoid St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce the serum concentration of ixazomib.
Take on an empty stomach. Food increases the absorption of ixazomib, take ixazomib dose at least one hour before and at least two hours after food.

[Moderate] ADJUST DOSING INTERVAL: Food may reduce the oral bioavailability of ixazomib.

A food effect study found that administration of a single 4 mg dose of ixazomib with a high-fat meal decreased ixazomib peak plasma concentration (Cmax) by 69% and systemic exposure (AUC) by 28%.

MANAGEMENT: Ixazomib should be taken at least one hour before or two hours after eating.

On days when both ixazomib and dexamethasone are administered, advise patients to separate dosing times, since dexamethasone should be taken with food while ixazomib should be taken on an empty stomach.