Leukemias, lymphomas, and other hematologic cancers:

Indications for: REZLIDHIA

Treatment of relapsed or refractory acute myeloid leukemia (AML) in adults with a susceptible IDH1 mutation, as detected by an FDA-approved test.

Adult Dosage:

Select patients based on the presence of IDH1 mutations. Swallow whole. Take at least 1hr before or 2hrs after a meal. 150mg twice daily (do not administer 2 doses within 8hrs) until disease progression or unacceptable toxicity. For those without disease progression or unacceptable toxicity: treat for a minimum of 6 months to allow time for clinical response. Dose modifications: see full labeling.

Children Dosage:

Not established.

Boxed Warning:

Differentiation syndrome.

REZLIDHIA Warnings/Precautions:

Obtain blood counts and blood chemistries including liver function tests prior to initiation, at least once weekly for the first 2 months, once every other week for the 3rd month, once in the 4th month, and once every other month thereafter. Withhold treatment if differentiation syndrome is suspected, and initiate systemic corticosteroids (eg, dexamethasone 10mg IV every 12hrs for at least 3 days) and hemodynamic monitoring until symptom resolution; initiate hydroxyurea if concomitant leukocytosis is observed. Withhold, reduce, or permanently discontinue if hepatic dysfunction occurs; monitor frequently for clinical symptoms (eg, fatigue, anorexia, right upper abdominal discomfort, dark urine, jaundice). Mild (total bilirubin ULN and any AST >ULN or total bilirubin >1–1.5xULN and any AST) or moderate (total bilirubin >1.5–3xULN and any AST) hepatic impairment: increased risk of differentiation syndrome; monitor closely. Severe renal impairment (CrCL 15–29mL/min), renal failure (CrCL <15mL/min), on dialysis, or severe hepatic impairment (total bilirubin >3xULN with any AST): dosage not established. Pregnancy. Nursing mothers: not recommended (during and for 2 weeks after the last dose). 

REZLIDHIA Classification:

Isocitrate dehydrogenase-1 (IDH1) inhibitor.

REZLIDHIA Interactions:

Antagonized by moderate or strong CYP3A inducers (eg, rifampin); avoid. Avoid concomitant use with sensitive CYP3A substrates; if unavoidable, monitor for loss of therapeutic effect of CYP3A substrates.

Adverse Reactions:

Increase AST/ALT, decreased K+, decreased sodium, increased ALP, nausea, increased creatinine, fatigue/malaise, arthralgia, constipation, increased lymphocytes, increased bilirubin, leukocytosis, increased uric acid, dyspnea, pyrexia, rash, increased lipase, mucositis, diarrhea, transaminitis; differentiation syndrome, hepatotoxicity.


N-dealkylation, demethylation, oxidative deamination followed by oxidation, mono-oxidation with subsequent glucuronidation. CYP3A4 (90%) with minor contributions from CYP2C8, CYP2C9, CYP1A2, CYP2C19. >93% plasma protein binding.

Drug Elimination:

Fecal (75%), renal (17%). Half-life: ~67 hours. 

Generic Drug Availability:


How Supplied: