glasdegib

Contraindicated in:

Blood donation should be avoided during and for ≥30 days following treatment;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Congenital long QT syndrome, HF, electrolyte abnormalities, or concurrent use of QT interval prolonging medications;
Severe renal impairment;
Rep: Women of reproductive potential and men with female partners of reproductive potential;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: atrial fibrillation, bradycardia, chest pain, peripheral edema, tachycardia, QT interval prolongation, VENTRICULAR ARRHYTHMIAS

Derm: rash, alopecia

F and E: hyperkalemia, hypokalemia, hypomagnesemia, hyponatremia

GI: abdominal pain, constipation, diarrhea, hyperbilirubinemia, ↑liver enzymes, metallic taste, mucositis, nausea, vomiting

GU: renal impairment, ↓fertility (males)

Hemat: anemia, bleeding, neutropenia, thrombocytopenia

Metab: ↓appetite, ↓weight

MS: ↑creatine kinase (CK), muscle spasm, pain

Neuro: dizziness, fatigue, headache

Resp: cough, dyspnea, pneumonia

Misc: fever

Interactions ⬆ ⬇

Drug-drug:

QT interval prolonging drugs may ↑ risk of QT interval prolongation and torsades de pointes; avoid concurrent use.
Strong CYP3A inhibitors, including ketoconazole, may ↑ levels and risk of toxicity; avoid concurrent use.
Strong CYP3A inducers, including rifampin, and moderate CYP3A inducers, including efavirenz, may ↓ levels and effectiveness; avoid concurrent use; if concurrent use with moderate CYP3A inducer unavoidable, ↓ glasdegib dosage.

Availability ⬆ ⬇

Tablets: 25 mg; 100 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 100 mg once daily on Day 1–28 of each 28-day cycle. Continue treatment for ≥6 cycles (in absence of unacceptable toxicity). Concurrent use of CYP3A inducer: If current dosage 100 mg once daily, ↑ to 200 mg once daily; if current dosage 50 mg once daily, ↑ to 100 mg once daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Binds to and inhibits smoothened, one of the transmembrane proteins involved in hedgehog signal transduction.

Therapeutic effects:

Improved survival.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: hedgehog pathway inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: 77% absorbed following oral administration; absorption ↓ by high-fat, high-calorie foods.

Distribution: Extensively distributed to tissues.

Protein Binding: 91%.

Metabolism/Excretion: Mostly metabolized in the liver by the CYP3A4 isoenzyme, and to some extent by CYP2C8 and UGT1A9. 42% excreted in urine (20% as unchanged drug), 42% excreted in feces (20% as unchanged drug).

Half-Life: 17.4 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	1.3–1.8 hr	24 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient to take glasdegib as directed. If vomiting occurs after dose, omit and take next scheduled dose next day. Take missed doses as soon as remembered and at least 12 hr before next scheduled dose; do not take 2 doses within 12 hr. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes.
Advise patient to contact their health care professional immediately if signs and symptoms of QT prolongation (feeling faint, light-headed, or dizzy or feeling heart beating irregularly or fast) occur.
Advise patient not to donate blood or blood products while taking glasdegib and for at least 30 days after the last dose because their blood or blood products might be given to a female of reproductive potential.
Advise males not to donate semen during glasdegib therapy and for at least 30 days after the last dose.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to avoid concurrent use of Rx, OTC, and herbal products without consulting health care professional.
Rep: May cause fetal harm. Advise female of reproductive potential to use effective contraception and to avoid breastfeeding during and for at least 30 days after last dose. Advise males with a female partner of reproductive potential to use effective contraception, including a condom, even after vasectomy, during and for at least 30 days after last dose. May impair male fertility.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

0069- Pfizer Laboratories Div Pfizer Inc
- 0069-0298- Daurismo
  - 0069-0298-60- 60 TABLET, FILM COATED in 1 BOTTLE (0069-0298-60)

0069- Pfizer Laboratories Div Pfizer Inc
- 0069-1531- Daurismo
  - 0069-1531-30- 30 TABLET, FILM COATED in 1 BOTTLE (0069-1531-30)

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Indications ⬇

Contraind./Precautions ⬆ ⬇