Instructions for Rezlidhia (Olutasidenib)

1. All names: Rezlidhia, Olutasidenib, FT-2102
2. Indications:
Rezlidhia (olutasidenib) is indicated for the treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) who have a predisposing isocitrate dehydrogenase-1 (IDH1) mutation detected by an FDA-approved test.
3. Usage and dosage:
1. Before treatment: Choose to receive Rezlidhia treatment based on the presence of IDH1 mutations in the blood or bone marrow.
2. Recommended dose: The recommended dose of Rezlidhia is 150 mg orally taken twice daily until disease progression or unacceptable toxicity occurs. Do not take 2 doses within 8 hours, take it on an empty stomach at least 1 hour before or 2 hours after a meal. For patients without disease progression or unacceptable toxicity, treat for at least 6 months to allow time for clinical response.
3. Dose adjustment: If a patient experiences adverse reactions when using Rezlidhia, the administration should be interrupted or the toxic dose should be reduced under the guidance of a doctor.
4. Adverse reactions:
In clinical trials of relapsed or refractory acute myeloid leukemia (AML), the most common (≥20%) adverse reactions (including laboratory abnormalities) include increased aspartate aminotransferase, increased alanine aminotransferase, decreased potassium, decreased sodium, alkaline Elevated sex phosphatase, nausea, elevated creatinine, fatigue/malaise, arthralgia, constipation, elevated lymphocytes, elevated bilirubin, leukocytosis, elevated uric acid, dyspnea, pyrexia, rash, elevated lipase, mucositis, diarrhea, and elevated transaminases.

5. Storage:

Rezlidhia is typically stored at 20°C to 25°C (68°F to 77°F); excursions allowed between 15°C and 30°C (59°F and 86°F).
6. Special groups:
1. Females: In embryo-fetal development studies, oral administration of Rezlidhia resulted in embryo-fetal lethality and altered fetal growth when administered to pregnant rats and rabbits during organogenesis. Therefore, females are advised not to breastfeed during treatment with Rezlidhia and for 2 weeks after the last dose.
7. Mechanism of action:
Olutasidenib is a small molecule inhibitor of mutant isocitrate dehydrogenase-1 (IDH1). In patients with acute myeloid leukemia, a predisposing IDH1 mutation is defined as a mutation that results in elevated 2-hydroxyglutarate (2-HG) levels in leukemia cells, and efficacy is predicted by: 1) clinically meaningful remission with the recommended dose of Rezlidhia, and/or 2) sustained inhibition of mutant IDH1 enzyme activity at the recommended dose of Rezlidhia concentration according to a validated method. The most common mutations in AML patients are R132H and R132C substitutions.
In vitro, Rezlidhia inhibits mutant IDH1 R132H, R132L, R132S, R132G, and R132C proteins; wild-type IDH1 or mutant IDH2 proteins are not inhibited. Rezlidhia inhibition of mutant IDH1 results in reduced 2-HG levels in in vitro and in vivo xenograft models.
After Rezlidhia is approved for marketing, there is little information about its price and other related information. Please consult the medical consultant for details.