ИКСАЗОМИБА ЦИТРАТ
ИКСАЗОМИБА ЦИТРАТ Uses, Dosage, Side Effects, Food Interaction and all others data.
ИКСАЗОМИБА ЦИТРАТ 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. ИКСАЗОМИБА ЦИТРАТ 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.
Trade Name | ИКСАЗОМИБА ЦИТРАТ |
Availability | Prescription only |
Generic | Ixazomib |
Ixazomib Other Names | Ixazomib |
Related Drugs | Revlimid, Velcade, Darzalex, Pomalyst, Ninlaro, Kyprolis |
Type | |
Formula | C14H19BCl2N2O4 |
Weight | Average: 361.03 Monoisotopic: 360.081492 |
Protein binding | 99% |
Groups | Approved, Investigational |
Therapeutic Class | |
Manufacturer | |
Available Country | Russia |
Last Updated: | September 19, 2023 at 7:00 am |
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Uses
ИКСАЗОМИБА ЦИТРАТ is a monoclonal antibody used with other medications to treat multiple myeloma in patients who have received one other therapy already.
ИКСАЗОМИБА ЦИТРАТ is indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received at least one prior therapy.
ИКСАЗОМИБА ЦИТРАТ is also used to associated treatment for these conditions: Multiple Myeloma (MM)
How ИКСАЗОМИБА ЦИТРАТ works
ИКСАЗОМИБА ЦИТРАТ 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. ИКСАЗОМИБА ЦИТРАТ 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: ИКСАЗОМИБА ЦИТРАТ 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.
ИКСАЗОМИБА ЦИТРАТ Drug Interaction
Moderate: carfilzomibUnknown: charcoal, contained in alcoholic beverages , olmesartan, sulfamethoxazole / trimethoprim, ubiquinone, copper gluconate, dexamethasone, glucose, diltiazem, apixaban, omega-3 polyunsaturated fatty acids, imatinib, chondroitin / glucosamine / methylsulfonylmethane, glycerin, sodium iodide, lenalidomide, cyanocobalamin, cholecalciferol, zoledronic acid
ИКСАЗОМИБА ЦИТРАТ Disease Interaction
Moderate: gastrointestinal toxicities, hepatic impairment, peripheral neuropathy, renal impairment, thrombocytopenia
Volume of Distribution
The steady-state volume of distribution is 543 L.
Elimination Route
After oral administration, the time to reach maximum concentration in plasma was 1 hour. The mean absolute oral bioavailability is 58%.
Half Life
Terminal half-life is 9.5 days.
Elimination Route
62% in urine and 22% in feces.
Innovators Monograph
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