Ixazomib

Ixazomib is a reversible proteasome inhibitor. Ixazomib preferentially binds and inhibits the chymotrypsin-like activity of the beta 5 subunit of the 20S proteasome.

• NINLARO is indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received at least one prior therapy. NINLARO is a proteasome inhibitor indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received at least one prior therapy.ICD-10: C90.00

• None. None.contraindicated

Recommended starting dose of 4 mg taken orally on Days 1, 8, and 15 of a 28-day cycle. ( 2.1 ) Dose should be taken at least one hour before or at least two hours after food. ( 2.1 ) 2.1 Dosing and Administration Guidelines NINLARO in combination with lenalidomide and dexamethasone The recommended starting dose of NINLARO is 4 mg administered orally once a week on Days 1, 8, and 15 of a 28-day treatment cycle. The recommended starting dose of lenalidomide is 25 mg administered daily on Days 1 through 21 of a 28-day treatment cycle. The recommended starting dose of dexamethasone is 40 mg administered on Days 1, 8, 15, and 22 of a 28-day treatment cycle. Table 1: Dosing Schedule for NINLARO taken with Lenalidomide and Dexamethasone ✔ Take medicine 28-Day Cycle (a 4-week cycle) Week 1 Week 2 Week 3 Week 4 Day 1 Days 2-7 Day 8 Days 9-14 Day 15 Days 16-21 Day 22 Days 23-28 NINLARO ✔ ✔ ✔ Lenalidomide ✔ ✔ Daily ✔ ✔ Daily ✔ ✔ Daily Dexamethasone ✔ ✔ ✔ ✔ For additional information regarding lenalidomide and dexamethasone, refer to their prescribing information. NINLARO should be taken once a week on the same day and at approximately the same time for the first three weeks of a four week cycle. The importance of carefully following all dosage instructions should be discussed with patients starting treatment. Instruct patients to take the recommended dosage as directed, because overdosage has led to deaths [see Overdosage (10) ] . NINLARO should be taken at least one hour before or at least two hours after food [see Clinical Pharmacology (12.3) ] .

Thrombocytopenia : Monitor platelet counts at least monthly during treatment and adjust dosing, as needed. ( 2.2 , 5.1 ) Gastrointestinal Toxicities : Adjust dosing for severe diarrhea, constipation, nausea, and vomiting, as needed. ( 2.2 , 5.2 ) Peripheral Neuropathy : Monitor patients for symptoms of peripheral neuropathy and adjust dosing, as needed. ( 2.2 , 5.3 ) Peripheral Edema : Monitor for fluid retention. Investigate for underlying causes, when appropriate. Adjust dosing, as needed. ( 2.2 , 5.4 ) Cutaneous Reactions : Monitor patients for rash and adjust dosing, as needed. ( 2.2 , 5.5 ) Thrombotic Microangiopathy : Monitor for signs and symptoms. Discontinue NINLARO if suspected. ( 5.6 ) Hepatotoxicity : Monitor hepatic enzymes during treatment. ( 5.7 ) Embryo-Fetal Toxicity : NINLARO can cause fetal harm. Advise patients of the potential risk to a fetus and to use effective non-hormonal contraception. ( 5.8 , 8.1 , 8.3 ) Increased Mortality in Patients Treated with NINLARO in the Maintenance Setting : Treatment of patients with NINLARO for multiple myeloma in the maintenance setting is not recommended outside of controlled trials. ( 5.9 ) 5.1 Thrombocytopenia Thrombocytopenia has been reported with NINLARO with platelet nadirs typically occurring between Days 14-21 of each 28-day cycle and recovery to baseline by the start of the next cycle [see Adverse Reactions (6.1) ] . Grade 3 thrombocytopenia was reported in 17% of patients in the NINLARO regimen and Grade 4 thrombocytopenia was reported in 13% in the NINLARO regimen.

The following adverse reactions are described in detail in other sections of the prescribing information: Thrombocytopenia [see Warnings and Precautions (5.1) ] Gastrointestinal Toxicities [see Warnings and Precautions (5.2) ] Peripheral Neuropathy [see Warnings and Precautions (5.3) ] Peripheral Edema [see Warnings and Precautions (5.4) ] Cutaneous Reactions [see Warnings and Precautions (5.5) ] Thrombotic Microangiopathy [see Warnings and Precautions (5.6) ] Hepatotoxicity [see Warnings and Precautions (5.7) ] The most common adverse reactions (≥20%) are thrombocytopenia, neutropenia, diarrhea, constipation, peripheral neuropathy, nausea, peripheral edema, rash, vomiting, and bronchitis. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Takeda Pharmaceuticals at 1-844-617-6468 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety population from the randomized, double-blind, placebo-controlled clinical study included 720 patients with relapsed and/or refractory multiple myeloma, who received NINLARO in combination with lenalidomide and dexamethasone (NINLARO regimen; N=361) or placebo in combination with lenalidomide and dexamethasone (placebo regimen; N=359).

Hepatic Impairment : Reduce the NINLARO starting dose to 3 mg in patients with moderate or severe hepatic impairment. ( 2.3 , 8.6 ) Renal Impairment : Reduce the NINLARO starting dose to 3 mg in patients with severe renal impairment or end-stage renal disease requiring dialysis. ( 2.4 , 8.7 ) Lactation : Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on its mechanism of action [see Clinical Pharmacology (12.1) ] and data from animal reproduction studies, NINLARO can cause fetal harm when administered to a pregnant woman. There are no available data on NINLARO use in pregnant women to evaluate drug-associated risk. Ixazomib caused embryo-fetal toxicity in pregnant rats and rabbits at doses resulting in exposures that were slightly higher than those observed in patients receiving the recommended dose (see Data ) . Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Data Animal Data In an embryo-fetal development study in pregnant rabbits there were increases in fetal skeletal variations/abnormalities (fused caudal vertebrae, number of lumbar vertebrae, and full supernumerary ribs) at doses that were also maternally toxic (≥0.3 mg/kg).

Metabolism

Absorption After oral administration, the median time to achieve peak ixazomib plasma concentrations was one hour. The mean absolute oral bioavailability was 58%, based on population PK analysis.

Overdosage, including fatal overdosage, has been reported in patients taking NINLARO. Manifestations of overdosage include adverse reactions reported at the recommended dosage [see Dosage and Administration (2.1) , Adverse Reactions (6.1) ] . Serious adverse reactions reported with overdosage include severe nausea, vomiting, diarrhea, aspiration pneumonia, multiple organ failure and death. In the event of an overdosage, monitor for adverse reactions and provide appropriate supportive care. NINLARO is not dialyzable.

• Nov 20, 2015NDANDA208462Takeda Pharms Usa

1. 1Plasma Cell Myeloma3,63613%
2. 2Death3,30112%
3. 3Diarrhoea3,14111%
4. 4Off Label Use2,95010%
5. 5Pneumonia1,9236.8%
6. 6Fatigue1,9106.7%
7. 7Nausea1,8356.5%
8. 8Neuropathy Peripheral1,4435.1%
9. 9Vomiting1,1033.9%
10. 10Rash1,0833.8%
11. 11Thrombocytopenia1,0443.7%
12. 12Platelet Count Decreased9943.5%
13. 13Constipation9633.4%
14. 14Asthenia9093.2%
15. 15Product Dose Omission Issue7952.8%

The 10 most recently updated of 163 ClinicalTrials.gov registrations naming Ixazomib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Venetoclax, MLN9708 (Ixazomib Citrate) and Dexamethasone for the Treatment of Relapsed or Refractory Light Chain Amyloidosis
  Active not recruiting · Phase 1 · Interventional · 24 enrolled · National Cancer Institute (NCI)
  NCT04847453updated 2026-06-11
• Ixazomib -Daratumumab Without Dexamethasone (IDara) in Elderly Relapse Refractory Multiple Myeloma
  Terminated · Phase 2 · Interventional · 55 enrolled · University Hospital, Caen
  NCT03757221updated 2026-05-13
• Study of Ixazomib and Romidepsin in Peripheral T-cell Lymphoma (PTCL)
  Terminated · Phase 1 · Phase 2 · Interventional · 11 enrolled · University of Michigan Rogel Cancer Center
  NCT03547700updated 2026-05-06
• Ibrutinib and Ixazomib Citrate in Treating Newly Diagnosed, Relapsed or Refractory Waldenstrom Macroglobulinemia
  Terminated · Phase 2 · Interventional · 21 enrolled · Mayo Clinic
  NCT03506373updated 2026-05-05
• Selinexor and Backbone Treatments of Multiple Myeloma Patients
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 300 enrolled · Karyopharm Therapeutics Inc
  NCT02343042updated 2026-05-04
• A Study of Ixazomib (NINLARO®) in Combination With Lenalidomide and Dexamethasone (IRD) for the Treatment of Participants With Multiple Myeloma (MM)
  Terminated · Phase 4 · Interventional · 141 enrolled · Takeda
  NCT03173092updated 2026-05-04
• Daratumumab, Bortezomib, and Dexamethasone Followed by Daratumumab, Ixazomib, and Dexamethasone in Treating Patients With Relapsed or Refractory Multiple Myeloma
  Active not recruiting · Phase 2 · Interventional · 40 enrolled · M.D. Anderson Cancer Center
  NCT03763162updated 2026-04-15
• Ixazomib + Pomalidomide + Dexamethasone In MM
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 52 enrolled · Omar Nadeem, MD
  NCT04094961updated 2026-03-05
• Ixazomib Citrate and Rituximab in Treating Patients With Indolent B-cell Non-Hodgkin Lymphoma
  Active not recruiting · Phase 2 · Interventional · 33 enrolled · University of Washington
  NCT02339922updated 2026-03-05
• A Study of Ninlaro in Real World Clinical Practice in China
  Completed · Observational · 482 enrolled · Takeda
  NCT04328662updated 2026-03-04

Frequently asked questions

How does Ixazomib work?

Ixazomib is a reversible proteasome inhibitor. Ixazomib preferentially binds and inhibits the chymotrypsin-like activity of the beta 5 subunit of the 20S proteasome.

What is Ixazomib used for?

According to FDA labeling, Ixazomib carries indications including: NINLARO is indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received at least one prior therapy. NINLARO is a proteasome inhibitor indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received at least one prior therapy.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Ixazomib?

Ixazomib is classified as Proteasome inhibitors, Proteasome Inhibitor, Proteasome Inhibitors, Increased Cellular Death.

What are the brand names for Ixazomib?

Ixazomib is marketed under brand names including Ninlaro.

What are the contraindications for Ixazomib?

Ixazomib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.