Rilzabrutinib: uses, dosing, side effects & brands

The following clinically important adverse reactions are described elsewhere in the labeling: Serious Infections [see Warnings and Precautions (5.1) ] Hepatotoxicity, Including Drug-Induced Liver Injury [ see Warnings and Precautions (5.2) ] Most common adverse reactions (incidence ≥10%) were diarrhea, nausea, headache, abdominal pain, and COVID-19. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Genzyme Corporation at 1-800-633-1610 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 of WAYRILZ was evaluated in a randomized, double-blind (DB), placebo-controlled, parallel-group study (LUNA-3), in which 202 adult patients with persistent or chronic ITP received either WAYRILZ (n=133) or placebo (n=69) [see Clinical Studies (14) ] . During the 24-week DB period, the median duration of WAYRILZ exposure was 98 days (range: 22 to 182). The most common adverse reactions (≥10%) were diarrhea, nausea, headache, abdominal pain, and COVID-19. Adverse reactions resulting in discontinuation of WAYRILZ included erythema nodosum, neutropenia, arthralgia, dyspepsia, headache, pain in…

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CYP3A Inhibitors: Avoid co-administration with moderate or strong CYP3A inhibitors. ( 7.1 ) CYP3A Inducers: Avoid co-administration with moderate or strong CYP3A inducers. ( 7.1 ) Gastric Acid Reducing Agents: Avoid co-administration with proton pump inhibitors (PPIs). WAYRILZ should be administered at least 2 hours before taking an antacid or H2 receptor antagonist. ( 7.1 ) 7.1 Effect of Other Drugs on WAYRILZ Strong and Moderate CYP3A Inhibitors Avoid concomitant use of WAYRILZ with strong or moderate CYP3A inhibitors. If a strong or moderate CYP3A inhibitor cannot be avoided, and these inhibitors will be used short term (such as anti-infectives for seven days or less), interrupt treatment with WAYRILZ. Avoid concomitant use of grapefruit, starfruit and products containing these fruits, and Seville oranges with WAYRILZ, as these are moderate and strong inhibitors of CYP3A. Rilzabrutinib is a CYP3A substrate. Concomitant use with a strong or moderate CYP3A inhibitor increases rilzabrutinib C max and AUC [see Clinical Pharmacology (12.3) ] , which increases the risk of WAYRILZ adverse reactions. Strong and Moderate CYP3A Inducers Avoid concomitant use of WAYRILZ with strong or moderate CYP3A inducers. Rilzabrutinib is a CYP3A substrate. Concomitant use with a strong or moderate CYP3A inducer decreases rilzabrutinib C max and AUC [see Clinical Pharmacology (12.3) ] , which may reduce WAYRILZ efficacy. Gastric Acid Reducing Agents Administer the dose of WAYRILZ at least 2 hours before administration of an antacid or histamine H2 receptor antagonist. Avoid concomitant use of proton pump inhibitors with WAYRILZ. Rilzabrutinib exhibits pH-dependent solubility. Acid reducing agents decrease rilzabrutinib exposure [see Clinical Pharmacology (12.3) ] , which may reduce WAYRILZ efficacy. 7.2 Effect of WAYRILZ on Other Drugs CYP3A Substrates Monitor for adverse reactions of the concurrently administered CYP3A substrate more frequently and consider dosage adjustment in accordance with the Prescribing Information of the CYP3A substrate. Rilzabrutinib is a moderate inhibitor of CYP3A and increases exposure of these substrates [see Clinical Pharmacology (12.3) ] , which increases the risk of adverse reactions related to these substrates. P-gp, BCRP, and OATP1B Substrates Monitor for adverse reactions of the concurrently administered P-gp, BCRP, or OATP1B substrate more frequently, unless otherwise recommended in the substrate Prescribing Information, when WAYRILZ is used concomitantly with P-gp, BCRP, or OATP1B substrates where minimal substrate concentration changes may lead to serious adverse reactions. Rilzabrutinib is an inhibitor of P-gp, BCRP and OATP1B in vitro . The effect of concomitant use of WAYRILZ with OATP1B and BCRP substrates has not been established in clinical studies. However, based on in vitro inhibitory potential [see Clinical Pharmacology (12.3) ] , concomitant use of WAYRILZ may increase the risk of adverse reactions related to these substrates.