nirogacestat (Ogsiveo)

Indications

• progressive, unresectable, recurrent, or refractory desmoid tumors in adults

Contraindications

• pregnancy: can cause fetal harm

Dosage

• 150 mg BID until disease progression or unacceptable tocixity

tablets 50 mg

Pharmacokinetics

• protein bindin 99%m 95% to albumin
• bioavailability 18%
• induces CYP2B6, CYP2C8, CYP2C9, & CYP2C19
• excreted in feces (38%), urine (17%), expirwd air (9.7%)
• mean terminal 1/2 life 23 hours

Adverse effects

• diarrhea (84%), nausea (54%), fatigue (51%)
• hypophosphatemia (42%)
• maculopapular rash (32%)
• cough
• alopecia
• increased serum transaminases, hypokalemia
• proteinuria, glucosuria
• transient ovarian dysfunction in most women of childbearing age

Drug interactions

• strong or moderate CYP3A inhibitors increase nirogacestat
• strong or moderate CYP3A inducers decrease nirogacestat
• antacids

Mechanism of action

• gamma secretase inhibitor

More general terms

• antineoplastic agent (chemotherapeutic agent)

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=46224413
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=121513889
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=163320817