REZLIDHIA: CONVENIENT ORAL DOSING WITH
A WELL-CHARACTERIZED SAFETY PROFILE
REZLIDHIA: CONVENIENT ORAL DOSING WITH A WELL-CHARACTERIZED SAFETY PROFILE
\Hello \ \Dr. \ \##accFname##,
\I wanted to share some safety and dosing information for
REZLIDHIA as a follow up to our recent conversation.
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.
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Please see additional Important Safety
Information below and Full Prescribing
Information, including Boxed WARNING.
Twice
Daily
Dosing
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The recommended dose for REZLIDHIA is one 150 mg capsule taken orally
twice daily until disease progression or unacceptable toxicity.1
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On
an Empty
Stomach
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REZLIDHIA should be taken on an empty stomach, at least 1 hour before
or 2 hours after a meal.1
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At
Least 6 Months of Treatment |
For patients without disease progression or unacceptable toxicity, treat for
a minimum of 6 months to allow time for clinical response.1
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Monitoring
Guidelines
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Assess blood counts and blood chemistries, including liver function tests,
prior to initiation of REZLIDHIA and for the duration of therapy.1
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REZLIDHIA DEMONSTRATED A
WELL-CHARACTERIZED SAFETY PROFILE
REZLIDHIA DEMONSTRATED A
WELL-CHARACTERIZED SAFETY PROFILE
Differentiation
syndrome occurred in 16% of patients
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Of the 25 patients who experienced differentiation syndrome, 19 (76%) recovered
after treatment or after dosage interruption1
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1 fatality occurred due to differentiation syndrome1
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QT
prolongation occurred in 8% (n=12) of patients
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No QT prolongation led to dose reduction or treatment discontinuation1,2
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Electrocardiogram monitoring is not required per the Prescribing Information.1,2
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No new or more frequent safety concerns were seen with long-term use of REZLIDHIA, based on the 5-year analysis3
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Here is some additional information that you may find useful.
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RIGEL ONECARE®
Find support for every step of treatment, including how to access REZLIDHIA, copay assistance, patient support services, and downloadable resources for you and your patients.
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Download the REZLIDHIA Patient Education Guide
Important information for patients about what to expect with REZLIDHIA when starting treatment.
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Download the REZLIDHIA Dosing Guide
Information on REZLIDHIA dosing and administration, monitoring, and dose modifications to manage potential adverse reactions.
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Download the Distribution Guide
Find information on REZLIDHIA distribution and pharmacy networks, and patient support services.
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Clinical Publication: Olutasidenib for Mutated IDH1 Acute Myeloid Leukemia: Final Five-Year Results From the Phase 2 Pivotal Cohort
Learn about the final 5-year efficacy and safety results from the REZLIDHIA pivotal cohort in the Journal of Hematology & Oncology.
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Clinical Publication: Olutasidenib (FT-2102) induces durable complete remissions in patients with relapsed or refractory IDH1-mutated AML
Review the results of the REZLIDHIA clinical trial in Blood Advances for details about efficacy, safety, and more.
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Download the Enrollment Form
Enroll patients in RIGEL ONECARE® for patient support services including benefits verification, prior authorizations, temporary and long-term drug supply, and adherence support. All Rigel programs are subject to eligibility requirements. Restrictions may apply.
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\Thank you for your time. I look forward to our next
appointment.
\Sincerely,
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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.
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
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