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Ixazomib

  • Other antineoplastics (differentiating agents, asparaginases, proteasome inhibitors)Other antineoplastics (differentiating agents, asparaginases, proteasome inhibitors)
  • High alertAn error with this medicine can cause serious harm: double checks and protocols are used.
  • Pregnancy: avoidAvoid in pregnancy. Can harm the fetus; effective contraception is used by women and by men with partners who could become pregnant, during treatment and for some months after…

Oral proteasome inhibitor, a capsule taken once a week with lenalidomide and dexamethasone for relapsed multiple myeloma.

Updated

Quick facts

Group
Other antineoplastics (differentiating agents, asparaginases, proteasome inhibitors)
Target
26S proteasome, β5 subunit (PSMB5) of the 20S core
Key effects
Diarrhoea · Rash · Swelling of the arms or legs
Monitor
Platelet count before each dose · Signs of neuropathy
ATC
L01XG03

No doses: the clinician sets them by the current guideline.

Mechanism of action

The crystal shows ixazomib in the active sites of the human 20S proteasome core.

Target in 3D: 26S proteasome, β5 subunit (PSMB5) of the 20S core. PDB structure 5LF7 (RCSB PDB, public domain). View the structure at RCSB PDB

Ixazomib is an oral peptide-analogue proteasome inhibitor that binds the β5 subunit (PSMB5) of the 20S proteasome. With the proteasome blocked, ubiquitin-tagged proteins, including cell-cycle and apoptosis regulators, are not broken down; misfolded protein builds up and myeloma cells die.

  1. Ixazomib binds the β5 subunit of the proteasome
  2. Ubiquitin-tagged proteins are not broken down
  3. Protein stress kills the myeloma cell

Indications

  • Multiple myeloma after at least one earlier therapy, with lenalidomide and dexamethasone. Multiple myeloma →

Adverse effects

Common

  • Diarrhoea, constipation, nausea, vomiting
  • Rash
  • Swelling of the arms or legs; back pain
  • Blurred vision, dry eyes, conjunctivitis

Contraindications

  • No absolute contraindications in the label apart from hypersensitivity; see the warnings

Key interactions

St John's wort
Interacts with ixazomib and is not started during treatment without medical advice.
Dexamethasone in the same regimen
Not taken at the same moment: dexamethasone is taken with food and ixazomib on an empty stomach.

What is monitored

  • Platelet count before each dose
  • Signs of neuropathy
  • Liver tests
  • Bowel habit, rash and swelling

Administration and safety

  • Oral capsule once a week on set days of each cycle, with water, on an empty stomach.
  • Swallowed whole: not opened, chewed or crushed.
  • Hazardous drug: if a capsule breaks, contact with skin, eyes, mouth or nose is avoided and the skin or eyes are washed.
  • If vomited, the dose is not repeated; the next dose is taken on the next scheduled day.

Pregnancy and breastfeeding

Avoid in pregnancy. Can harm the fetus; effective contraception is used by women and by men with partners who could become pregnant, during treatment and for some months after, and breastfeeding is avoided.

Nursing care

  • Teach the weekly schedule clearly, separate from the lenalidomide and dexamethasone days and timings.
  • Check platelets and ask about bruising or bleeding.
  • Ask about numbness, tingling or burning in the hands and feet.
  • Ask about St John's wort and liver or kidney disease.

Pharmacokinetics

Absorption
Oral capsule taken on an empty stomach, at least an hour before or two hours after food.
Half-life
Very long, about 9.5 days, which allows weekly dosing.

Test yourself

Think of the answer, then tap the question to see it.

What makes ixazomib different from bortezomib and carfilzomib?

It is taken by mouth, once a week.

With which two drugs is ixazomib combined?

Lenalidomide and dexamethasone.

Which blood count is checked before each ixazomib dose?

Platelets, because thrombocytopenia is a key toxicity.

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More Pharmacology questions →

Connections

← Back to the class: Other antineoplastics (differentiating agents, asparaginases, proteasome inhibitors)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Ixazomib: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2016); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); Human 20S proteasome complex with Ixazomib at 2.0 Angstrom (RCSB Protein Data Bank, 2016).

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Representative model, for educational purposes only.