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Drug overview for REZLIDHIA (olutasidenib):
Generic name: olutasidenib (oh-LOO-ta-SID-e-nib)
Drug class: Antineoplastic - Isocitrate Dehydrogenase-1 Inhibitor (IDH1)
Therapeutic class: Antineoplastics
Olutasidenib, an isocitrate dehydrogenase-1 (IDH1) inhibitor, is an antineoplastic agent.
No enhanced Uses information available for this drug.
Generic name: olutasidenib (oh-LOO-ta-SID-e-nib)
Drug class: Antineoplastic - Isocitrate Dehydrogenase-1 Inhibitor (IDH1)
Therapeutic class: Antineoplastics
Olutasidenib, an isocitrate dehydrogenase-1 (IDH1) inhibitor, is an antineoplastic agent.
No enhanced Uses information available for this drug.
DRUG IMAGES
REZLIDHIA 150 MG CAPSULE
The following indications for REZLIDHIA (olutasidenib) have been approved by the FDA:
Indications:
Acute myeloid leukemia with isocitrate dehydrogenase-1 (IDH1) mutation
Professional Synonyms:
IDH1 mutation-positive acute myeloid leukemia
Indications:
Acute myeloid leukemia with isocitrate dehydrogenase-1 (IDH1) mutation
Professional Synonyms:
IDH1 mutation-positive acute myeloid leukemia
The following dosing information is available for REZLIDHIA (olutasidenib):
If toxicity occurs, olutasidenib may require dosage reduction, temporary withholding of the dose, or discontinuation. See Table 1 for recommended actions based on adverse reaction type and severity.
Table 1. Dosage Modifications for Adverse Reactions to Olutasidenib.
Adverse Reaction Recommended Action Differentiation syndrome If differentiation syndrome is suspected, withhold olutasidenibuntil signs and symptoms improve. Administer systemic corticosteroids and initiate hemodynamic monitoring until symptom resolution and for a minimum of 3 days. Resume at 150 mg twice daily aft er resolution.
If a recurrence is suspected, withhold olutasidenib and institute treatment per above guidance. After symptom resolution, resume at a reduced dosage of 150 mg once daily for a minimum of 7 days, after which it can be increased to 150 mg twi ce daily. Noninfectious leukocytosis Initate treatment with hydroxyurea as per standard practices.
Taper hydroxyurea only after leukocytosis improves or resolves. Grade 3 hepatotoxicity Withhold olutasideniband monitor liver function tests twice per week until laboratory values have returned to baseline or grade 1 toxicity. Resume at a reduced dosage of 150 mg once daily and continue monitoring; may increase to 150 mg twice daily if hepa totoxicity resolves to baseline for at least 28 days.If
hepatotoxicity (grade 3) recurs at 150 mg once daily, discontinue olutasidenib. Grade 4 hepatotoxicity or AST or ALT Permanently discontinue >3x ULN and total bilirubin >2x ULN olutasidenib. and alkaline phosphatase <2x ULN in the absence of a clear alternative explanation Other grade 3 or higher toxicity Interrupt olutasidenib until considered related to treatment toxicity resolves to grade 2 or lower.
Resume at 150 mg once daily; may increase to 150 mg twice daily if toxicities resolved to grade 1 or lower for at least 1 week. If grade 3 or higher toxicity recurs at 150 mg once daily, discontinueolutasidenib.
Table 1. Dosage Modifications for Adverse Reactions to Olutasidenib.
Adverse Reaction Recommended Action Differentiation syndrome If differentiation syndrome is suspected, withhold olutasidenibuntil signs and symptoms improve. Administer systemic corticosteroids and initiate hemodynamic monitoring until symptom resolution and for a minimum of 3 days. Resume at 150 mg twice daily aft er resolution.
If a recurrence is suspected, withhold olutasidenib and institute treatment per above guidance. After symptom resolution, resume at a reduced dosage of 150 mg once daily for a minimum of 7 days, after which it can be increased to 150 mg twi ce daily. Noninfectious leukocytosis Initate treatment with hydroxyurea as per standard practices.
Taper hydroxyurea only after leukocytosis improves or resolves. Grade 3 hepatotoxicity Withhold olutasideniband monitor liver function tests twice per week until laboratory values have returned to baseline or grade 1 toxicity. Resume at a reduced dosage of 150 mg once daily and continue monitoring; may increase to 150 mg twice daily if hepa totoxicity resolves to baseline for at least 28 days.If
hepatotoxicity (grade 3) recurs at 150 mg once daily, discontinue olutasidenib. Grade 4 hepatotoxicity or AST or ALT Permanently discontinue >3x ULN and total bilirubin >2x ULN olutasidenib. and alkaline phosphatase <2x ULN in the absence of a clear alternative explanation Other grade 3 or higher toxicity Interrupt olutasidenib until considered related to treatment toxicity resolves to grade 2 or lower.
Resume at 150 mg once daily; may increase to 150 mg twice daily if toxicities resolved to grade 1 or lower for at least 1 week. If grade 3 or higher toxicity recurs at 150 mg once daily, discontinueolutasidenib.
Olutasidenib is administered orally as a capsule. Swallow whole; do not break, open, or chew the capsules. Olutasidenib should be taken on an empty stomach at least 1 hour before or 2 hours after a meal.
Administer the drug at about the same time each day; do not administer 2 doses within 8 hours. If a dose is vomited, do not administer a replacement dose; wait until the next scheduled dose is due. If a dose is missed or not taken at the usual time, administer the dose as soon as possible and at least 8 hours prior to the next scheduled dose.
Return to the normal schedule the following day. Store capsules at 20-25degreesC (excursions permitted between 15-30degreesC).
Administer the drug at about the same time each day; do not administer 2 doses within 8 hours. If a dose is vomited, do not administer a replacement dose; wait until the next scheduled dose is due. If a dose is missed or not taken at the usual time, administer the dose as soon as possible and at least 8 hours prior to the next scheduled dose.
Return to the normal schedule the following day. Store capsules at 20-25degreesC (excursions permitted between 15-30degreesC).
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| REZLIDHIA 150 MG CAPSULE | Maintenance | Adults take 1 capsule (150 mg) by oral route 2 times per day |
No generic dosing information available.
The following drug interaction information is available for REZLIDHIA (olutasidenib):
There are 0 contraindications.
There are 1 severe interactions.
These drug interactions can produce serious consequences in most patients. Actions required for severe interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration scheduling, and providing additional patient monitoring. Review the full interaction monograph for more information.
| Drug Interaction | Drug Names |
|---|---|
| Olutasidenib/Strong and Moderate CYP3A4 Inducers SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Strong and moderate CYP3A4 inducers may increase the metabolism of olutasidenib by CYP3A4.(1) CLINICAL EFFECTS: The concurrent use of strong and moderate CYP3A4 inducers and olutasidenib may result in decreased levels and clinical effectiveness of olutasidenib.(1) PREDISPOSING FACTORS: Induction effects may be more likely with regular use of the inducer for longer than 1-2 weeks. PATIENT MANAGEMENT: Avoid concomitant use of strong and moderate CYP3A4 inducers with olutasidenib.(1) DISCUSSION: Coadministration of multiple doses of rifampin (a strong CYP3A4 inducer) decreased olutasidenib area-under-curve (AUC) and maximum concentration (Cmax) by 80% and 43%, respectively.(1) Strong and moderate CYP3A4 inducers linked to this monograph include: apalutamide, barbiturates, belzutifan, bosentan, carbamazepine, cenobamate, dabrafenib, dipyrone, efavirenz, elagolix, encorafenib, enzalutamide, etravirine, fosphenytoin, ivosidenib, lesinurad, lorlatinib, lumacaftor, mavacamten, mitapivat, mitotane, modafinil, nafcillin, pacritinib, pexidartinib, phenobarbital, phenytoin, primidone, repotrectinib, rifabutin, rifampin, rifapentine, St. John's wort, sotorasib, telotristat, thioridazine, and tovorafenib.(2) |
ASA-BUTALB-CAFFEINE-CODEINE, ASCOMP WITH CODEINE, AUGTYRO, BOSENTAN, BRAFTOVI, BUTALB-ACETAMINOPH-CAFF-CODEIN, BUTALBITAL, BUTALBITAL-ACETAMINOPHEN, BUTALBITAL-ACETAMINOPHEN-CAFFE, BUTALBITAL-ASPIRIN-CAFFEINE, CAMZYOS, CARBAMAZEPINE, CARBAMAZEPINE ER, CARBATROL, CEREBYX, DILANTIN, DILANTIN-125, DONNATAL, DUZALLO, EFAVIRENZ, EFAVIRENZ-EMTRIC-TENOFOV DISOP, EFAVIRENZ-LAMIVU-TENOFOV DISOP, EPITOL, EQUETRO, ERLEADA, ETRAVIRINE, FIORICET, FIORICET WITH CODEINE, FOSPHENYTOIN SODIUM, INTELENCE, LORBRENA, LUMAKRAS, LYSODREN, MITOTANE, MODAFINIL, MYSOLINE, NAFCILLIN, NAFCILLIN SODIUM, OJEMDA, ORIAHNN, ORILISSA, ORKAMBI, PENTOBARBITAL SODIUM, PHENOBARBITAL, PHENOBARBITAL SODIUM, PHENOBARBITAL-BELLADONNA, PHENOBARBITAL-HYOSC-ATROP-SCOP, PHENOHYTRO, PHENYTEK, PHENYTOIN, PHENYTOIN SODIUM, PHENYTOIN SODIUM EXTENDED, PRIFTIN, PRIMIDONE, PROVIGIL, PYRUKYND, RIFABUTIN, RIFADIN, RIFAMPIN, SEZABY, SYMFI, TAFINLAR, TALICIA, TEGRETOL, TEGRETOL XR, TENCON, THIORIDAZINE HCL, THIORIDAZINE HYDROCHLORIDE, TIBSOVO, TRACLEER, TURALIO, VONJO, WELIREG, XCOPRI, XERMELO, XTANDI |
There are 0 moderate interactions.
The following contraindication information is available for REZLIDHIA (olutasidenib):
Drug contraindication overview.
*None.
*None.
There are 1 contraindications.
Absolute contraindication.
| Contraindication List |
|---|
| Lactation |
There are 1 severe contraindications.
Adequate patient monitoring is recommended for safer drug use.
| Severe List |
|---|
| Pregnancy |
There are 3 moderate contraindications.
Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.
| Moderate List |
|---|
| Child-pugh class A hepatic impairment |
| Child-pugh class B hepatic impairment |
| Disease of liver |
The following adverse reaction information is available for REZLIDHIA (olutasidenib):
Adverse reaction overview.
The most common adverse reactions (occurring in >=20% of patients) are increased AST,increased ALT, increased alkaline phosphatase, increased creatinine, increased lymphocytes, increased bilirubin, increased lipase, increased uric acid, decreased potassium, decreased sodium, nausea, fatigue/malaise, arthralgia, constipation, leukocytosis, dyspnea, pyrexia, rash, mucositis, diarrhea, and transaminitis.
The most common adverse reactions (occurring in >=20% of patients) are increased AST,increased ALT, increased alkaline phosphatase, increased creatinine, increased lymphocytes, increased bilirubin, increased lipase, increased uric acid, decreased potassium, decreased sodium, nausea, fatigue/malaise, arthralgia, constipation, leukocytosis, dyspnea, pyrexia, rash, mucositis, diarrhea, and transaminitis.
There are 12 severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Elevated serum lipase Hyperbilirubinemia Hyperuricemia Hypokalemia Hyponatremia Increased alkaline phosphatase Increased aspartate transaminase Leukocytosis Lymphocytosis |
Cholangitis Cholestasis Differentiation syndrome |
| Rare/Very Rare |
|---|
| None. |
There are 16 less severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Arthralgia Constipation Diarrhea Dyspnea Fatigue Fever Malaise Nausea Skin rash Stomatitis |
Acute abdominal pain Anorexia Cough Edema Headache disorder Vomiting |
| Rare/Very Rare |
|---|
| None. |
The following precautions are available for REZLIDHIA (olutasidenib):
Safety and effectiveness of olutasidenib have not been established in pediatric patients.
Contraindicated
Severe Precaution
Management or Monitoring Precaution
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
Based on animal embryo-fetal toxicity studies,olutasidenib may cause fetal harm when administered to a pregnant woman. There are no available data onolutasidenib use in pregnant women to evaluate for a drug-associated risk. In embryo-fetal development studies, oralolutasidenib resulted in embryo-fetal death and altered fetal growth when administered to pregnant rats and rabbits during the period of organogenesis at exposures up to 10 times and 0.7
times, respectively, the human exposure at the recommended daily dose. Advise pregnant women of the potential risk to a fetus.
times, respectively, the human exposure at the recommended daily dose. Advise pregnant women of the potential risk to a fetus.
There are no data on the presence ofolutasidenib or its metabolites in human milk, the effects on the breast-fed child, or the effects on milk production. Because many drugs are excreted in human milk, and due to the potential for adverse reactions in a breast-fed child, advise women not to breast-feed during treatment witholutasidenib and for 2 weeks after the last dose.
Among the 153 patients with relapsed/refractory IDH1-mutated AML treated witholutasidenib in clinical trials, 76% were>=65 years of age and 31% were>=75 years of age. No overall differences in effectiveness were observed between patients >=65 years of age and younger patients. Compared to patients <65 years of age, an increased incidence of hepatotoxicity and hypertension was observed in patients>=65 years of age.
The following prioritized warning is available for REZLIDHIA (olutasidenib):
WARNING: Olutasidenib may cause a serious (possibly fatal) condition called differentiation syndrome. Get medical help right away if you develop any signs of differentiation syndrome, such as fever, cough, shortness of breath, decreased urination, rapid weight gain, or swelling of arms/legs.
WARNING: Olutasidenib may cause a serious (possibly fatal) condition called differentiation syndrome. Get medical help right away if you develop any signs of differentiation syndrome, such as fever, cough, shortness of breath, decreased urination, rapid weight gain, or swelling of arms/legs.
The following icd codes are available for REZLIDHIA (olutasidenib)'s list of indications:
| Acute myeloid leukemia with IDh1 mutation | |
| C92.0 | Acute myeloblastic leukemia |
| C92.00 | Acute myeloblastic leukemia, not having achieved remission |
| C92.02 | Acute myeloblastic leukemia, in relapse |
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