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CRENIGACESTAT
Generic Name: CRENIGACESTAT
ABSTRACT -
Crenigacestat is a selective gamma-secretase inhibitor that blocks cleavage of Notch receptors, thereby suppressing Notch signaling, which drives proliferation and survival of tumor cells in desmoid tumors and T-cell acute lymphoblastic leukemia (T-ALL). It is under clinical investigation as a single agent and in combination with other agents for Notch-driven malignancies.
DOSAGE -
Administered orally per clinical trial protocol; intermittent dosing schedules investigated to manage GI toxicity.
SIDE EEFECTS -
- Diarrhea (class effect — goblet cell hyperplasia)
- Nausea and vomiting
- Fatigue
- Anorexia
- Mucositis
ALLERGIC REACTIONS -
(These symptoms may indicate an allergic reaction and require medical attention.)
- Drug hypersensitivity reactions
- Rash or urticaria
- Anaphylaxis (rare)
- Stevens-Johnson syndrome (rare)
DRUG INTERACTIONS-
- Strong CYP3A4 inhibitors increase crenigacestat exposure
- CYP3A4 inducers reduce efficacy
- Avoid concurrent GI-toxic agents
PREAUTONS–
- Prophylactic antidiarrheal therapy recommended
- Monitor liver enzymes
- Intermittent dosing schedules to mitigate GI toxicity
- Pregnancy: teratogenic risk; contraception required
WARNINGS –
- Severe diarrhea — dose-limiting GI toxicity requiring loperamide and dose reduction
- Hepatotoxicity reported
- Embryo-fetal toxicity — not for use in pregnancy
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