IDHIFA Film-coated tablet (2020)

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Celgene Corporation

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BOXED WARNING SECTION

WARNING: DIFFERENTIATION SYNDROME Patients treated with IDHIFA have experienced symptoms of differentiation syndrome, which can be fatal if not treated. Symptoms may include fever, dyspnea, acute respiratory ...

1. Indications and Usage

1.1 Acute Myeloid Leukemia IDHIFA is indicated for the treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) with an isocitrate dehydrogenase-2 (IDH2) mutation as detected ...

2. Dosage and Administration

2.1 Patient Selection Select patients for the treatment of AML with IDHIFA based on the presence of IDH2 mutations in the blood or bone marrow [see Indications and Usage (1.1) and Clinical Studies ...

3. Dosage Forms and Strengths

IDHIFA is available in the following tablet strengths: 50-mg tablet: Pale yellow to yellow oval-shaped film-coated tablet debossed ENA on one side and 50 on the other side. 100-mg tablet: Pale yellow to ...

4. Contraindications

None.

5. Warnings and Precautions

5.1 Differentiation Syndrome In the clinical trial, 14% of patients treated with IDHIFA experienced differentiation syndrome, which may be life-threatening or fatal if not treated. Differentiation syndrome ...

6. Adverse Reactions

The following clinically significant adverse reactions are described elsewhere in the labeling: Differentiation Syndrome [see Warnings and Precautions (5.1)]

6.1. Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another ...

8.1. Pregnancy

Risk Summary Based on animal embryo-fetal toxicity studies, IDHIFA can cause fetal harm when administered to a pregnant woman. There are no available data on IDHIFA use in pregnant women to inform a drug-associated ...

8.2. Lactation

Risk Summary There are no data on the presence of enasidenib or its metabolites in human milk, the effects on the breastfed child, or the effects on milk production. Because many drugs are excreted in ...

8.3. Females and Males of Reproductive Potential

Pregnancy Testing Based on animal embryo-fetal toxicity studies, IDHIFA can cause fetal harm when administered to a pregnant woman [see Use in Specific Populations (8.1)]. Obtain a pregnancy test ...

8.4. Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

8.5. Geriatric Use

No dosage adjustment is required for IDHIFA based on age. In the clinical study, 61% of 214 patients were aged 65 years or older, while 24% were older than 75 years. No overall differences in effectiveness ...

11. Description

IDHIFA (enasidenib) is an inhibitor of isocitrate dehydrogenase-2 (IDH2) enzyme. Enasidenib is available as the mesylate salt with the chemical name: 2-methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]6{[2-(trifluoromethyl)pyridin-4-yl]amino}-1,3,5-triazin-2-yl)amino]propan-2-ol ...

12.1. Mechanism of Action

Enasidenib is a small molecule inhibitor of the isocitrate dehydrogenase 2 (IDH2) enzyme. Enasidenib targets the mutant IDH2 variants R140Q, R172S, and R172K at approximately 40-fold lower concentrations ...

12.2. Pharmacodynamics

Cardiac Electrophysiology The potential for QTc prolongation with enasidenib was evaluated in an open-label study in patients with advanced hematologic malignancies with an IDH2 mutation. Based on the ...

12.3. Pharmacokinetics

The peak plasma concentration (Cmax) is 1.4 mcg/mL [% coefficient of variation (CV%) 50.2] after a single dose of 100 mg, and 13.1 mcg/mL (CV% 44.8) at steady state for 100 mg daily. The area ...

13.1. Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenicity studies have not been performed with enasidenib. Enasidenib was not mutagenic in an in vitro bacterial reverse mutation (Ames) assay. Enasidenib was not clastogenic in an in vitro human ...

14. Clinical Studies

14.1 Acute Myeloid Leukemia The efficacy of IDHIFA was evaluated in an open-label, single-arm, multicenter, two-cohort clinical trial (Study AG221-C-001, NCT01915498) of 199 adult patients with relapsed ...

16.1. How Supplied

50-mg tablet: Pale yellow to yellow oval-shaped film-coated tablet debossed ENA on one side and 50 on the other side. 30-count bottles of 50-mg tablets with a desiccant canister (NDC 59572-705-30) 100-mg ...

16.2. Storage and Handling

Store at 20°C-25°C (68°F-77°F); excursions permitted between 15°C-30°C (59°F-86°F) [see USP Controlled Room Temperature]. Keep the bottle tightly closed. Store in the original bottle (with a desiccant ...

17. Patient Counseling Information

Advise the patient to read the FDA-approved patient labeling (Medication Guide). Differentiation Syndrome Advise patients on the risks of developing differentiation syndrome as early as 1 day and during ...