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Developed under the direction and sponsorship of Rigel Pharmaceuticals, Inc.
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INDICATION
REZLIDHIA is indicated for the treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) with a susceptible isocitrate dehydrogenase-1 (IDH1) mutation as detected by an FDA-approved test.
SELECT IMPORTANT SAFETY INFORMATION
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WARNING: DIFFERENTIATION SYNDROME
Differentiation syndrome, which can be fatal, can occur with REZLIDHIA treatment. Symptoms may include dyspnea, pulmonary infiltrates/
pleuropericardial effusion, kidney injury, hypotension, fever, and weight gain. If differentiation syndrome is suspected, withhold REZLIDHIA and initiate treatment with corticosteroids and hemodynamic monitoring until symptom resolution.
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Please see additional Important Safety Information below and Full Prescribing Information, including Boxed WARNING.
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WHEN PATIENTS WITH mIDH1 AML PROGRESS AFTER TREATMENT WITH INTENSIVE CHEMOTHERAPY, WHAT’S NEXT?
WHEN PATIENTS WITH mIDH1 AML PROGRESS AFTER TREATMENT WITH INTENSIVE CHEMOTHERAPY, WHAT’S NEXT?
Outcomes after intensive chemotherapy can be poor for patients with AML. For those who progress and have an IDH1 mutation, consider treating next with REZLIDHIA as their first IDH1 inhibitor.1-3
IDH1 inhibitors are recommended by the National Comprehensive Cancer Network® (NCCN®) as treatment options for patients with IDH1-mutated AML in the relapsed or refractory setting, which may occur following prior intensive induction therapy.4
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REZLIDHIA PROVIDED A CLINICALLY MEANINGFUL RESPONSE WITH DURABLE, COMPLETE REMISSION
REZLIDHIA PROVIDED A CLINICALLY MEANINGFUL RESPONSE WITH DURABLE, COMPLETE REMISSION
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Efficacy Results in Patients with Relapsed
or
Refractory
IDH1-mutated
AML (N=147)5-8*
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Endpoint
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Results with REZLIDHIA
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Patients achieving CR/CRh†
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35% (95% CI: 27-43)
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Patients achieving CRc (CR/CRh/CRi)
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45%
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Median duration of CR/CRh
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25.3 months (95% CI: 13.5-NR)
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Median time to CR or CRh
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1.9 months (95% CI: 1-2.8)
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View the full efficacy of REZLIDHIA from the pivotal trial and long-term analysis.
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Rezlidhia response rates as the first
IDH1 inhibitor following intensive chemotherapy treatment progression‡
Rezlidhia response rates as the first IDH1 inhibitor following intensive chemotherapy treatment progression‡
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Findings from a subgroup analysis of 13 patients treated with an intensive chemotherapy-based regimen prior to treatment with REZLIDHIA.8
Clinical Response Rates (n=13)8
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For patients with mIDH1 AML who relapse or are refractory to initial treatment, choose REZLIDHIA as the first R/R targeted therapy
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IMPORTANT SAFETY
INFORMATION (CONT’D)
WARNINGS AND
PRECAUTIONS
Differentiation Syndrome
REZLIDHIA can cause differentiation syndrome. In
the clinical trial of REZLIDHIA in patients with relapsed or
refractory AML, differentiation syndrome occurred in 16% of
patients, with grade 3 or 4 differentiation syndrome occurring
in 8% of patients treated, and fatalities in 1% of patients.
Differentiation syndrome is associated with rapid proliferation
and differentiation of myeloid cells and may be life-threatening
or fatal. Symptoms of differentiation syndrome in patients
treated with REZLIDHIA included leukocytosis, dyspnea, pulmonary
infiltrates/pleuropericardial effusion, kidney injury, fever,
edema, pyrexia, and weight gain. Of the 25 patients who
experienced differentiation syndrome, 19 (76%) recovered after
treatment or after dose interruption of REZLIDHIA.
Differentiation syndrome occurred as early as 1 day and up to 18
months after REZLIDHIA initiation and has been observed with or
without concomitant leukocytosis.
If differentiation syndrome is suspected,
temporarily withhold REZLIDHIA and initiate systemic
corticosteroids (e.g., dexamethasone 10 mg IV every 12 hours)
for a minimum of 3 days and until resolution of signs and
symptoms. If concomitant leukocytosis is observed, initiate
treatment with hydroxyurea, as clinically indicated. Taper
corticosteroids and hydroxyurea after resolution of symptoms.
Differentiation syndrome may recur with premature
discontinuation of corticosteroids and/or hydroxyurea treatment.
Institute supportive measures and hemodynamic monitoring until
improvement; withhold dose of REZLIDHIA and consider dose
reduction based on recurrence.
Hepatotoxicity
REZLIDHIA can cause hepatotoxicity, presenting as
increased alanine aminotransferase (ALT), increased aspartate
aminotransferase (AST), increased blood alkaline phosphatase,
and/or elevated bilirubin. Of 153 patients with relapsed or
refractory AML who received REZLIDHIA, hepatotoxicity occurred
in 23% of patients; 13% experienced grade 3 or 4 hepatotoxicity.
One patient treated with REZLIDHIA in combination with
azacitidine in the clinical trial, a combination for which
REZLIDHIA is not indicated, died from complications of
drug-induced liver injury. The median time to onset of
hepatotoxicity in patients with relapsed or refractory AML
treated with REZLIDHIA was 1.2 months (range: 1 day to 17.5
months) after REZLIDHIA initiation, and the median time to
resolution was 12 days (range: 1 day to 17 months). The most
common hepatotoxicities were elevations of ALT, AST, blood
alkaline phosphatase, and blood bilirubin.
Monitor patients frequently for clinical symptoms
of hepatic dysfunction such as fatigue, anorexia, right upper
abdominal discomfort, dark urine, or jaundice. Obtain baseline
liver function tests prior to initiation of REZLIDHIA, at least
once weekly for the first two months, once every other week for
the third month, once in the fourth month, and once every other
month for the duration of therapy. If hepatic dysfunction
occurs, withhold, reduce, or permanently discontinue REZLIDHIA
based on recurrence/severity.
ADVERSE
REACTIONS
The most common (≥20%) adverse reactions,
including laboratory abnormalities, were aspartate
aminotransferase increased, alanine aminotransferase increased,
potassium decreased, sodium decreased, alkaline phosphatase
increased, nausea, creatinine increased, fatigue/malaise,
arthralgia, constipation, lymphocytes increased, bilirubin
increased, leukocytosis, uric acid increased, dyspnea, pyrexia,
rash, lipase increased, mucositis, diarrhea and transaminitis.
DRUG
INTERACTIONS
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Avoid concomitant use of REZLIDHIA with strong
or moderate CYP3A inducers. |
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Avoid concomitant use of REZLIDHIA with
sensitive CYP3A substrates unless otherwise
instructed in the substrates prescribing
information. If concomitant use is unavoidable,
monitor patients for loss of therapeutic effect
of these drugs. |
LACTATION
Advise women not to breastfeed during treatment with REZLIDHIA and for 2 weeks after the last dose.
GERIATRIC USE
No overall differences in effectiveness were observed between patients 65 years and older and younger
patients. Compared to patients younger than 65 years of age, an increase in incidence of hepatotoxicity and hypertension was
observed in patients ≥65 years of age.
HEPATIC IMPAIRMENT
In patients with mild or moderate hepatic impairment, closely monitor for increased probability of differentiation syndrome.
Please see REZLIDHIAhcp.com for Full
Prescribing Information, including Boxed WARNING.
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REFERENCES:
1. Niscola P, Gianfelici V, Catalano G, et al. Acute myeloid leukemia in older patients: from new biological insights to targeted therapies. Curr Oncol. 2024;31(11):6632-6658. Error in Figure 1 legend. Correction. Curr Oncol. 2025;32(7):386. doi:10.3390/curroncol32070386 2. Bataller A, Kantarjian H, Bazinet A, et al. Outcomes and genetic dynamics of acute myeloid leukemia at first relapse. Haematologica. 2024;109(11):3543-3556. doi:10.3324/haematol.2024.285057 3. van der Maas NG, Breems D, Klerk CPW, et al. A revised prognostic model for patients with acute myeloid leukemia and first relapse. Blood Adv. 2025;9(15):3853-3864. doi:10.1182 bloodadvances.2025015797 4. Referenced with permission from the NCCN Clinical Practice Guidelines in Oncology (NCCN Guidelines®) for Acute Myeloid Leukemia V.3.2026. © National Comprehensive Cancer Network, Inc. 2025. All rights reserved. Accessed December 11, 2025. To view the most recent and complete version of the guideline, go online to NCCN.org. NCCN makes no warranties of any kind whatsoever regarding their content, use or application and disclaims any responsibility for their application or use in any way. 5. REZLIDHIA® Package insert. Rigel Pharmaceuticals, Inc; 2022. 6. de Botton S, Fenaux P, Yee K, et al. Olutasidenib (FT-2102) induces durable complete remissions in patients with relapsed or refractory IDH1-mutated AML. Blood Adv. 2023;7(13):3117-3127. doi:10.1182/bloodadvances.2022009411 7. Cortes J, Curti A, Fenaux P, et al. Olutasidenib for mutated IDH1 acute myeloid leukemia: final five-year results from the phase 2 pivotal cohort. J Hematol Oncol. 2025;18(1):102. doi:10.1186/s13045-025-01751-w 8. Data on file, Rigel Pharmaceuticals, Inc. January 2025.
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© 2026 Rigel Pharmaceuticals, Inc. All rights reserved. REZ_AML-25080 0226
REZLIDHIA and RIGEL ONECARE are registered trademarks of Rigel Pharmaceuticals, Inc.
RIGEL ONECARE is a patient support center sponsored by Rigel Pharmaceuticals, Inc.
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