rilzabrutinib

Contraindicated in:

Severe renal impairment;
Moderate or severe hepatic impairment;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Rep: Women of reproductive potential;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

EENT: nasopharyngitis

GI: abdominal pain, diarrhea, nausea, HEPATOTOXICITY, dyspepsia, vomiting

Hemat: neutropenia

MS: arthralgia

Neuro: headache, dizziness

Resp: cough

Misc: INFECTION

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A inhibitors, including ritonavir, or moderate CYP3A inhibitors, including erythromycin, fluconazole, or verapamil, may ↑ levels and risk of toxicity; avoid concurrent use. If concurrent use necessary and use of CYP3A inhibitors is short-term in nature, can interrupt therapy with rilzabrutinib.
Strong CYP3A inducers, including rifampin, or moderate CYP3A inducers, including efavirenz or rifabutin, may ↓ levels and effectiveness; avoid concurrent use.
Antacids, H2 receptor antagonists, and proton pump inhibitors can ↓ levels and effectiveness. Avoid concurrent use with proton pump inhibitors; separate administration from antacids or H₂ receptor antagonists by ≥2 hr.
May ↑ levels and risk of toxicity of CYP3A substrates, including midazolam.
May ↑ levels and risk of toxicity of P-glycoprotein substrates, breast cancer resistance protein (BCRP) substrates, or organic anion-transporting polypeptide (OATP) 1B substrates.

Drug-Natural Products:

St. John's wort may ↓ levels and effectiveness; avoid concurrent use.

Drug-Food:

Grapefruit, starfruit, and Seville oranges may ↑ levels and risk of toxicity; avoid concurrent use.

Availability ⬆ ⬇

Route/Dosage ⬆ ⬇

PO (Adults ): 400 mg twice daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Inhibits Bruton tyrosine kinase, which inhibits B-cell activation and decreases production of autoantibodies.

Therapeutic effects:

Sustained increase in platelet concentrations.

Classifications ⬆ ⬇

Therapeutic Classification: none assigned

Pharmacologic Classification: kinase inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: 4.7% absorbed following oral administration; absorption ↓ by high-fat foods.

Distribution: Widely distributed to tissues.

Protein Binding: 97.5%.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A isoenzyme. Primarily excreted in the feces (86%; 9% as unchanged drug); 5% excreted in urine; 6% excreted in bile.

Half-Life: 1.6–4.5 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2 hr	12 hr

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
Advise patient that if a dose is missed, take as soon as possible on the same day and ≥2 hr apart from the next scheduled dose. Take ≥2 hr before antacid or H₂ receptor antagonist.
Instruct patient to store rilzabrutinib at room temperature in original package to protect from light and moisture.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care provider before taking other medications.
Advise patient to avoid eating grapefruit, starfruit, and Seville oranges during therapy.
Advise patient to notify health care provider if any signs/symptoms of infection or hepatotoxicity (abdominal pain, dark urine, jaundice) occur.
Rep: Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected. Advise women of reproductive potential to use effective contraception during therapy and for 1 wk after last dose and not to breastfeed during therapy or for 1 wk after last dose.

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Indications ⬇

Contraind./Precautions ⬆ ⬇