Important Safety
Information Full Prescribing
Information

REZUROCK (belumosudil) tablets logo REZUROCK (belumosudil) tablets logo

THE ROCKstar STUDY

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The ROCKstar (KD025-213) study

REZUROCK demonstrated significant efficacy in patients after failure of ≥2 prior lines of systemic therapy1

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REZUROCK achieved clinically meaningful and statistically significant ORR with the FDA-approved dose of 200 mg once daily1

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Clinically meaningful responses were achieved across all affected organs, even those with fibrotic manifestations2

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CR, with the 200-mg once-daily dose, was achieved in all affected organ systems2

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Clinically significant FFS and OS rates3

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Clinically meaningful improvements (≥7-point reduction) in LSS summary score from baseline were observed, showing an increase in patient functioning and well-being1

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CS reductions and discontinuations were observed in 64% and 20% of patients, respectively2

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CNI reductions and discontinuations were observed in 42% and 17% of patients, respectively3

STATISTICALLY SIGNIFICANT ORRa FOLLOWING TREATMENT WITH REZUROCK 200 mg ONCE DAILY1,4,5

bar graph of overall response rate (ORR), 75%, with REZUROCK 200 mg once daily bar graph of overall response rate (ORR), 75%, with REZUROCK 200 mg once daily

aProportion of patients who achieved CR or PR according to the 2014 NIH cGVHD Consensus Criteria.1

bThe final FDA interpretation of the ROCKstar study omitted 1 patient from the REZUROCK 200-mg once-daily arm. As a result, there are minor differences between the ROCKstar publication, where n=66, and the Prescribing Information, where n=65.

cStatistical significance was achieved if the lower bound of the 95% CI of ORR exceeded 30%.4

REZUROCK ALSO DEMONSTRATED CLINICALLY MEANINGFUL ORRs ACROSS KEY SUBGROUPS IN THE 200-mg ONCE-DAILY ARM3

EARLYd cGVHD DIAGNOSIS

89%

(n/N=32/36)

SEVERE cGVHD

76%

(n/N=35/46)

cGVHD INVOLVING ≥4 ORGANS

73%

(n/N=24/33)

>3 PRIOR LINES OF SYSTEMIC THERAPY

70%

(n/N=21/30)

REFRACTORY TO THEIR PRIOR LINE OF SYSTEMIC THERAPY

75%

(n/N=9/12)

PRIOR IBRUTINIB THERAPY

73%

(n/N=16/22)

PRIOR RUXOLITINIB THERAPY

65%

(n/N=13/20)

dEarly diagnosis was defined as <28 months from time of initial diagnosis to enrollment.3

RESPONSES BY ORGAN SYSTEM WITH REZUROCK 200 mg ONCE DAILY IN THE mITT POPULATION (N=66)3

bar graph of complete and partial responses (CR and PR) by organ system in modified intent-to-treat (mITT) responders, including the upper GI tract, esophagus, lower GI tract, mouth, joints/fascia, liver, skin, eyes and lungs
bar graph of complete and partial responses (CR and PR) by organ system in modified intent-to-treat (mITT) responders, including the upper GI tract, esophagus, lower GI tract, mouth, joints/fascia, liver, skin, eyes and lungs

CR was seen in all organs, including the lungs, skin, eyes and liver.2

Responses were observed across all affected organs, even those with fibrotic manifestations.2

Clinically significant responses across multiple measures2

graphic showing the time to response was as early as 4 weeks, 63% of responses were observed between weeks 4 and 8, 94% of responses were observed by week 24, approximately 61% of responders demonstrated a sustained response for 20 or more weeks, and there was no death or new systemic therapy initiation in 62% (95% CI, 46-74) of the responder population at 12 months graphic showing the time to response was as early as 4 weeks, 63% of responses were observed between weeks 4 and 8, 94% of responses were observed by week 24, approximately 61% of responders demonstrated a sustained response for 20 or more weeks, and there was no death or new systemic therapy initiation in 62% (95% CI, 46-74) of the responder population at 12 months

ePrespecified secondary end point; not powered to show statistical significance.

fThe responder population in the 200-mg once-daily arm was n=49.3

gBased on a final analysis by the FDA (n=65).

FFS3,e,h

graph showing the FFS rate was 73% at 6 months and 57% at 12 months graph showing the FFS rate was 73% at 6 months and 57% at 12 months graph showing the FFS rate was 73% at 6 months and 57% at 12 months

ePrespecified secondary end point; not powered to show statistical significance.

hFFS was defined as the absence of relapse, nonrelapse mortality or a need for additional systemic therapy.2

OS3,e,i

graph showing the 2-year OS rate was 89% graph showing the 2-year OS rate was 89%

ePrespecified secondary end point; not powered to show statistical significance.

iOS was defined as the time from the first dose of REZUROCK to the date of death due to any cause.3

LSS SUMMARY score: RATE OF clinically meaningful improvement (≥7-point reduction)1

52%

OF PATIENTSj

(95 CI, 40-65)

Clinically meaningful improvements (≥7-point reduction) in LSSe,k summary score were observed from baseline, showing an increase in patient functioning and well-being.1

ePrespecified secondary end point; not powered to show statistical significance.

jBased on a final analysis by the FDA (n=65).

kThe LSS is a 30-item, 7-subscale symptom scale and QOL measurement tool that evaluates the AEs of cGVHD in the categories of skin, vitality, lung, nutritional status, psychological functioning, eye and mouth.6

CS DOSE reductions and discontinuations2,e

Doses were
reduced in

64%

of patients.

THE MEAN Dose
was reduced by

43%

in patients.

A mean CS dose reduction of 49% was observed in responders.

Treatment was discontinued in

20%

of patients.

CNI DOSE reductions and discontinuations3,e

Doses were
reduced in

42%

of patients.

Treatment was
discontinued in

17%

of patients.

ePrespecified secondary end point; not powered to show statistical significance.

TOLERABILITY IS KEY

in allowing patients to realize the full benefit of therapy.7

SEE THE SAFETY PROFILE FOR REZUROCK

AE, adverse event; cGVHD, chronic graft-versus-host disease; CNI, calcineurin inhibitor; CR, complete response; CS, corticosteroid; DOR, duration of response; FDA, US Food and Drug Administration; FFS, failure-free survival; GI, gastrointestinal; LSS, Lee Symptom Scale; mITT, modified intent-to-treat; MOA, mechanism of action; ORR, overall response rate; OS, overall survival; PR, partial response.

References: 1. REZUROCK. Package insert. Kadmon Pharmaceuticals, LLC; 2021. 2. Cutler CS, Lee SJ, Arai S, et al. Belumosudil for chronic graft-versus-host disease (cGVHD) after 2 or more prior lines of therapy: the ROCKstar study. Blood. 2021;blood.2021012021. doi:10.1182/blood.2021012021. 3. Data on file 1. Kadmon Pharmaceuticals, LLC; 2021. 4. Data on file 2. Kadmon Pharmaceuticals, LLC; 2019. 5. Data on file. Kadmon Pharmaceuticals, LLC; 2021. 6. Lee SJ, Nguyen TD, Onstad L, et al. Success of immunosuppressive treatments in patients with chronic graft-versus-host disease. Biol Blood Marrow Transplant. 2018;24(3):555-562. doi:10.1016/j.bbmt.2017.10.042 7. Broadening the definition of tolerability in cancer clinical trials to better measure the patient experience. Friends of Cancer Research. Published October 24, 2018. Accessed July 27, 2021. https://www.focr.org/sites/default/files/Comparative Tolerability Whitepaper_FINAL.pdf

Indication

REZUROCKTM (belumosudil) is indicated for the treatment of adult and pediatric patients 12 years and older with chronic graft-versus-host disease (chronic GVHD) after failure of at least two prior lines of systemic therapy.

IMPORTANT SAFETY INFORMATION

Warnings and Precautions

Embryo-Fetal Toxicity: Based on findings in animals and its mechanism of action, REZUROCK can cause fetal harm when administered to a pregnant woman. Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential and males with female partners of reproductive potential to use effective contraception during treatment with REZUROCK and for at least one week after the last dose

Adverse Reactions

The most common (≥ 20%) adverse reactions, including laboratory abnormalities, were infections, asthenia, nausea, diarrhea, dyspnea, cough, edema, hemorrhage, abdominal pain, musculoskeletal pain, headache, phosphate decreased, gamma glutamyl transferase increased, lymphocytes decreased, and hypertension

Permanent discontinuation of REZUROCK due to adverse reactions occurred in 18% of patients. The adverse reactions which resulted in permanent discontinuation of REZUROCK in > 3% of patients included nausea (4%). Adverse reactions leading to dose interruption occurred in 29% of patients. The adverse reactions leading to dose interruption in ≥ 2% were infections (11%), diarrhea (4%), and asthenia, dyspnea, hemorrhage, hypotension, liver function test abnormal, nausea, pyrexia, edema, and renal failure with (2% each)

Monitor total bilirubin, aspartate aminotransferase (AST), and alanine aminotransferase (ALT) at least monthly

Drug Interactions

Strong CYP3A Inducers: Coadministration of REZUROCK with strong CYP3A inducers decreases belumosudil exposure, which may reduce the efficacy of REZUROCK. Increase the dosage of REZUROCK to 200 mg twice daily when coadministered with strong CYP3A inducers

Proton Pump Inhibitors: Coadministration of REZUROCK with proton pump inhibitors decreases belumosudil exposure, which may reduce the efficacy of REZUROCK. Increase the dosage of REZUROCK to 200 mg twice daily when coadministered with proton pump inhibitors

Use in Specific Populations

Pregnancy: Based on findings from animal studies and the mechanism of action, REZUROCK can cause fetal harm when administered to pregnant women. There are no available human data on REZUROCK use in pregnant women to evaluate for a drug-associated risk. Advise pregnant women and females of reproductive potential of the potential risk to the fetus

Lactation: There are no data available on the presence of belumosudil or its metabolites in human milk or the effects on the breastfed child, or milk production. Because of the potential for serious adverse reactions from belumosudil in the breastfed child, advise lactating women not to breastfeed during treatment with REZUROCK and for at least one week after the last dose

Pediatric Use: The safety and effectiveness of REZUROCK have been established in pediatric patients 12 years and older. The safety and effectiveness of REZUROCK in pediatric patients less than 12 years old have not been established

Geriatric Use: Of the 186 patients with chronic GVHD in clinical studies of REZUROCK, 26% were 65 years and older. No clinically meaningful differences in safety or effectiveness of REZUROCK were observed in comparison to younger patients

Renal and Hepatic Impairment: Treatment with REZUROCK has not been studied in patients with pre-existing severe renal or hepatic impairment. For patients with pre-existing severe renal or hepatic impairment, consider the risks and potential benefits before initiating treatment with REZUROCK

Please see full Prescribing Information for additional Important Safety Information.

You are encouraged to report side effects of prescription drugs to the FDA. Visit www.FDA.gov/medwatch or call 1-800-FDA-1088. You may also contact Kadmon Pharmaceuticals, LLC, at 1-877-377-7862 to report side effects.

© 2021 Kadmon Pharmaceuticals, LLC.
All Rights Reserved.
KAD25000025 09/21

Indication

REZUROCKTM (belumosudil) is indicated for the treatment of adult and pediatric patients 12 years and older with chronic graft-versus-host disease (chronic GVHD) after failure of at least two prior lines of systemic therapy.

Important safety information Warnings and Precautions

Embryo-Fetal Toxicity: Based on findings in animals and its mechanism of action, REZUROCK can cause fetal harm when administered to a pregnant woman. Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential and males with female partners of reproductive potential to use effective contraception during treatment with REZUROCK and for at least one week after the last dose

Indication & Important safety information

REZUROCKTM (belumosudil) is indicated for the treatment of adult and pediatric patients 12 years and older with chronic graft-versus-host disease (chronic GVHD) after failure of at least two prior lines of systemic therapy.