|
|
Developed under the direction and sponsorship of Rigel Pharmaceuticals, Inc.
|
|
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
|
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.
|
Please see additional
Important Safety
Information
below and Full Prescribing
Information, including Boxed
WARNING.
|
|
REZLIDHIA PROVIDED A DURABLE, COMPLETE REMISSION
|
|
Efficacy Results in Patients with Relapsed
or
Refractory
IDH1-mutated
AML (N=147)1-4*
|
|
Endpoint
|
Results with REZLIDHIA
|
|
Patients achieving CR/CRh†
|
35% (95% CI: 27-43)
|
|
Patients achieving CRc (CR/CRh/CRi)
|
45%
|
|
Median duration of CR/CRh
|
25.3 months (95% CI: 13.5-NR)
|
|
Median time to CR or CRh
|
1.9 months (95% CI: 1-2.8)
|
|
|
View the full efficacy of REZLIDHIA from the pivotal trial and long-term analysis.
|
|
REZLIDHIA RESPONSE RATES AS THE FIRST IDH1 INHIBITOR FOLLOWING STANDARD OF CARE TREATMENT PROGRESSION
REZLIDHIA RESPONSE RATES AS THE FIRST IDH1 INHIBITOR FOLLOWING STANDARD OF CARE TREATMENT PROGRESSION
|
|
Subgroup analysis after a venetoclax-based regimen or intensive chemotherapy
Prior Venetoclax-based Regimen (n=12)5
Median duration of previous venetoclax-based treatment was 6.7 months (range: 2-34 months)3
Prior Intensive Chemotherapy (n=13)4‡
Results in these high-risk subgroups are consistent
with the overall patient population (N=147): 45% achieve CRc2-7
|
Results in these high-risk subgroups
are consistent with the overall patient population (N=147): 45% achieve CRc2-7
|
|
|
For patients with mIDH1 AML who relapse or are refractory to initial treatment, choose REZLIDHIA as the first R/R targeted therapy
|
|
Learn more about REZLIDHIA
|
|
|
|
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
|
• |
Avoid concomitant use of REZLIDHIA with strong
or moderate CYP3A inducers. |
|
• |
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.
|
|
REFERENCES:
1. REZLIDHIA®. Package insert. Rigel Pharmaceuticals, Inc; 2022.
2. 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
3. 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
4. Data on file, Rigel Pharmaceuticals, Inc. January 2025.
5. 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 (supplemental data). J Hematol Oncol. 2025; https://link.springer.com/article/10.1186/s13045-025-01751-w#Sec20
6. Maiti A, Rausch CR, Cortes JE, et al. Outcomes of relapsed or refractory acute myeloid leukemia after frontline hypomethylating agent and venetoclax regimens. Haematologica. 2021;106(3):894-898. doi:10.3324/haematol.2020.252569
7. 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
|
© 2026 Rigel Pharmaceuticals, Inc. All rights reserved. REZ_AML-25081 0226
REZLIDHIA and RIGEL ONECARE are registered trademarks of Rigel Pharmaceuticals, Inc.
RIGEL ONECARE is a patient support center sponsored by Rigel Pharmaceuticals, Inc.
611 Gateway Blvd, Suite 900, South San Francisco, CA 94080
|
|
|
