Drug Safety-related Labeling Changes (SrLC)

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Drug Safety-related Labeling Changes (SrLC) Database

ANDA	Abbreviated New Drug Application
BLA	Biologics License Application
CDER	Center for Drug Evaluation and Research
MG	Medication Guide
NDA	New Drug Application
PCI	Patient Counseling Information
PI	Patient Information
PLR	Physician Labeling Rule
PLLR	Pregnancy and Lactation Labeling Rule
Italics	For the most part, italics indicate an FDA comment such as: Additions and/or revisions underlined These italics usually appear at the beginning of the section. In some cases, italics may be an inherent part of the label, and will most often appear in the body of the section.
Underlines	Any text that is underlined indicates text that has been added or revised. There are exceptions where underlining occurs in a section subtitle or heading. This is the case when there is just one word underlined in the body of the text.

Sections

BW	Box Warning
WP	Warnings and Precautions all in one section (PLR-format) Warnings as one section (pre-PLR format) Precautions as one section (pre-PLR format)
AR	Adverse Reactions (in pre-PLR format, this may be a subheading under precautions).
DI	Drug Interactions (in pre-PLR format, this may be a subheading under precautions).
USP	Use in Specific Populations (Inclusive on one or more of the following: Pregnancy; Lactation (PLLR- format); Nursing Mothers (pre-PLLR format); Females and Males of Reproductive Potential (PLLR format only); Pediatric Use, Geriatric Use, Renal Impairment, Hepatic Impairment, Sex, Race (these last six may be a subheading of precautions if label in pre-PLLR format.
PCI/PI/MG	Patient Counseling Information (PLR format only) - summarizes the information that a health care provider should convey to a patient (or caregiver when applicable) when a counseling discussion is taking place (e.g., a physician prescribing a drug during an office visit, a nurse providing discharge instructions at a hospital, or a pharmacist conveying information at a pharmacy). Patient Information - FDA approved patient labeling. Medication Guide - paper handouts that come with many prescription medicines. The guides address issues that are specific to particular drugs and drug classes, and they contain FDA-approved information that can help patients avoid serious adverse events.

Only NDAs and CDER regulated BLAs are included in this database. ANDAs are not included.

Applications that remain active, even if the product has been discontinued, undergo safety-related labeling changes.

REZUROCK (NDA-214783)

(BELUMOSUDIL MESYLATE)

Safety-related Labeling Changes Approved by FDA Center for Drug Evaluation and Research (CDER)

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01/15/2026 (SUPPL-12)

Approved Drug Label (PDF)

7 Drug Interactions

7.1 Effect of Other Drugs on REZUROCK

Additions and/or revisions underlined:

Proton Pump Inhibitors

Belumosudil exhibits pH-dependent solubility. Concomitant use of REZUROCK with proton pump inhibitors decreases belumosudil exposure [see Clinical Pharmacology (12.3)], which may reduce the efficacy of REZUROCK. Increase the dosage of REZUROCK when used concomitantly with proton pump inhibitors [see Dosage and Administration (2.3)].

Strong CYP3A Inducers

Belumosudil is a CYP3A substrate. Concomitant use of REZUROCK with strong CYP3A inducers decreases belumosudil exposure [see Clinical Pharmacology (12.3)], which may reduce the efficacy of REZUROCK. Increase the dosage of REZUROCK when used concomitantly with strong CYP3A inducers [see Dosage and Administration (2.3)].

7.2 Effect of REZUROCK on Other Drugs

Additions and/or revisions underlined:

BCRP and OATP1B1 Substrates

Avoid concomitant use with drugs that are BCRP substrates where possible. If used together, monitor patients more frequently for adverse reactions and decrease the BCRP substrates dosage(s) in accordance with the respective Prescribing Information.

Belumosudil is a BCRP inhibitor. Concomitant use of REZUROCK with BCRP substrates increases their plasma concentrations [see Clinical Pharmacology (12.3)], which may increase the risk of adverse reactions related to these substrates.

Belumosudil is an OATP1B1 inhibitor. Concomitant use of REZUROCK with OATP1B1 substrates may increase their plasma concentrations. Monitor patients more frequently for adverse reactions of these substrates and decrease the OATP1B1 substrates dosage(s) in accordance with the respective Prescribing Information [see Clinical Pharmacology (12.3)].

Certain CYP1A2 Substrates

Avoid concomitant use of REZUROCK with drugs that are sensitive CYP1A2 substrates, for which minimal concentration changes may lead to serious toxicities. If concomitant use cannot be avoided, decrease the CYP1A2 substrate dosage(s) in accordance with the respective Prescribing Information.

Belumosudil is a CYP1A2 inhibitor. Concomitant use of REZUROCK with sensitive CYP1A2 substrates (e.g., caffeine) is predicted to increase CYP1A2 substrate exposure [see Clinical Pharmacology (12.3)], which may increase the risk of adverse reactions related to these substrates.

Certain CYP3A Substrates

Avoid concomitant use of REZUROCK with drugs that are sensitive CYP3A substrates, for which minimal concentration changes may lead to serious toxicities. If concomitant use cannot be avoided, decrease the CYP3A substrate dosage(s) in accordance with the respective Prescribing Information.

Belumosudil is a CYP3A inhibitor. Concomitant use of REZUROCK with sensitive CYP3A substrates (e.g., midazolam) is predicted to increase CYP3A substrate exposure [see Clinical Pharmacology (12.3)], which may increase the risk of adverse reactions related to these substrates.

Certain UGT1A1 Substrates

Avoid concomitant use of REZUROCK with drugs that are UGT1A1 substrates, for which minimal concentration changes may lead to serious toxicities. If concomitant use cannot be avoided, decrease the UGT1A1 substrates dosage(s) in accordance with the respective Prescribing Information.

Belumosudil is a UGT1A1 inhibitor. Concomitant use of REZUROCK with a UGT1A1 substrate decreased plasma concentrations of the glucuronide metabolite of the UGT1A1 substrate [see Clinical Pharmacology (12.3)]. Concomitant use of belumosudil with other UGT1A1 substrates may increase their plasma concentrations, which may increase the risk of adverse reactions related to these substrates.

Certain P-gp Substrates

Avoid concomitant use of REZUROCK with drugs that are P-gp substrates, for which minimal concentration changes may lead to serious toxicities. If concomitant use cannot be avoided, decrease the P-gp substrates dosage(s) in accordance with the respective Prescribing Information.

Belumosudil is a P-gp inhibitor. Concomitant use of REZUROCK with P-gp substrates increased their plasma concentrations [see Clinical Pharmacology (12.3)], which may increase the risk of adverse reactions related to these substrates.

12/30/2024 (SUPPL-7)

Approved Drug Label (PDF)

8 Use in Specific Populations

8.1 Pregnancy

Additions and/or revisions underlined:

Risk Summary

… In animal reproduction studies, administration of belumosudil to pregnant rats and rabbits during the period of organogenesis resulted in adverse developmental outcomes, including alterations to growth, embryo-fetal mortality, and embryo-fetal malformations at maternal exposures (AUC) approximately Greater than or equal to1.4 (rat) and greater than or equal to 0.08 (rabbit) times the human exposure (AUC) at the recommended dose (see Data). Advise pregnant women and females of reproductive potential of the potential risk to the fetus.

…

Data

Animal data

… The exposure (AUC) at 50 mg/kg/day in rats is approximately 1.4 times the human exposure at the recommended dose of 200 mg.

…

Malformations included those in the tail (short), ribs (branched, fused or deformed), sternebrae (fused), and neural arches (fused, misaligned, and deformed). The exposure (AUC) at 50 mg/kg/day in rabbits is approximately 0.08 times the human exposure at the recommended dose of 200 mg.

04/10/2024 (SUPPL-5)

Approved Drug Label (PDF)

7 Drug Interactions

7.2 Effect of REZUROCK on Other Drugs

Newly added subsection:

Certain UTG1A1 substrates

Avoid coadministration of REZUROCK with UGT1A1 substrates, for which minimal concentration changes may lead to serious toxicities. If coadministration cannot be avoided, decrease the UGT1A1 substrates dosage(s) in accordance with the respective Prescribing Information.

REZUROCK is an inhibitor of UGT1A1. Coadministration of REZUROCK with a UGT1A1 substrate decreased plasma concentrations of the glucuronide metabolite [see Clinical Pharmacology (12.3)], which may increase the risk of adverse reactions related to sensitive substrates of UGT1A1.

Certain P-gp, OATP1B1, and BCRP substrates

Avoid coadministration of REZUROCK with P-gp, OATP1B1, and BCRP substrates, for which minimal concentration changes may lead to serious toxicities. If coadministration cannot be avoided, decrease the P-gp, OATP1B1, and BCRP substrates dosage(s) in accordance with the respective Prescribing Information.

REZUROCK is an inhibitor of P-gp, OATP1B1, and BCRP. Coadministration of REZUROCK with P-gp, OATP1B1, and BCRP substrates increased their plasma concentrations [see Clinical Pharmacology (12.3)], which may increase the risk of adverse reactions related to these substrates.

11/09/2023 (SUPPL-3)

Approved Drug Label (PDF)

8 Use in Specific Populations

8.6 Renal Impairment

(Newly added subsection)

Treatment with REZUROCK has not been studied in patients with pre-existing severe renal impairment. For patients with pre-existing severe renal impairment, consider the risks and potential benefits before initiating treatment with REZUROCK [see Dosage and Administration (2.1) and Clinical Pharmacology (12.3)].

8.7 Hepatic Impairment

(Newly added subsection)

Avoid use in patients with moderate hepatic impairment (Child-Pugh B) or severe hepatic impairment (Child-Pugh C) without liver GVHD [see Dosage and Administration (2.4), Clinical Pharmacology (12.3)].

No dosage adjustment is recommended for patients with mild hepatic impairment (Child-Pugh A) [see Dosage and Administration (2.4), Clinical Pharmacology (12.3)].