Thursday, July 7, 2022
HomeUncategorizedDaurismo (Glasdegib Maleate)

Daurismo (Glasdegib Maleate)

Daurismo (Glasdegib Maleate)

Daurismo is a prescription medicine that is used with the medicine cytarabine to treat newly-diagnosed Acute myeloid leukemia (AML) in adults who:

  • are 75 years of age or older, or have other medical conditions that prevent the use of standard chemotherapy

It is not known if Daurismo is safe and effective in children.

What are the possible side effects of Daurismo?

Daurismo can cause serious side effects, including:

  • See “What is the most important information I should know about Daurismo?”
  • Changes in the electrical activity of your heart are called QT prolongation. QT prolongation can cause irregular heartbeats that can be life-threatening. Tell your healthcare provider right away if you feel faint, lightheaded, dizzy, or feel your heart beating irregularly or fast during treatment with Daurismo.

The most common side effects of Daurismo with cytarabine include:

  • low red blood cell count (anemia)
  • low platelet count
  • tiredness
  • shortness of breath
  • bleeding
  • decreased appetite
  • fever with low white blood cell count
  • muscle pain
  • nausea
  • swelling of arms or legs
  • changes in taste
  • pain or sores in your mouth or throat
  • constipation
  • rash

Daurismo may affect fertility in males. 

Daurismo (glasdegib) is a potent small molecule inhibitor of Smoothened (SMO) for oral use. It is formulated with the maleate salt of glasdegib. The molecular formula for glasdegib maleate is C25H26N6O5. The molecular weight for glasdegib maleate is 490.51 Daltons. The chemical name of glasdegib maleate is 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate. The molecular structure is shown below:

DAURISMO™ (glasdegib) Structural Formula Illustration

Glasdegib maleate is a white to pale colored powder with pKa values of 1.7 and 6.1. The aqueous solubility of glasdegib maleate is 1.7 mg/mL.

Daurismo (glasdegib) is supplied as a film-coated tablet for oral use containing either 100 mg glasdegib (equivalent to 131.1 mg glasdegib maleate) or 25 mg of glasdegib (equivalent to 32.8 mg glasdegib maleate) together with microcrystalline cellulose, dibasic calcium phosphate anhydrous, sodium starch glycolate, and magnesium stearate as inactive ingredients in the tablet. The film-coating consists of Opadry II® Beige (33G170003) and Opadry II® Yellow (33G120011) containing: hypromellose, titanium dioxide, lactose monohydrate, macrogol, triacetin, iron oxide yellow, and iron oxide red.

Daurismo can cause serious side effects, including:

  1. See “What is the most important information I should know about Daurismo?”
  2. Changes in the electrical activity of your heart called QT prolongation. QT prolongation can cause irregular heartbeats that can be life-threatening. Tell your healthcare provider right away if you feel faint, lightheaded, dizzy, or feel your heart beating irregularly or fast during treatment with this.

The most common side effects of Daurismo with cytarabine include:

  • low red blood cell count (anemia)
  • low platelet count
  • tiredness
  • shortness of breath
  • bleeding
  • decreased appetite
  • fever with low white blood cell count
  • muscle pain
  • nausea
  • swelling of arms or legs
  • changes in taste
  • pain or sores in your mouth or throat
  • constipation
  • rash

Daurismo may affect fertility in males. Talk to your healthcare provider if this is a concern for you.

DESCRIPTION

Daurismo (glasdegib) is a potent small molecule inhibitor of Smoothened (SMO) for oral use. It is formulated with the maleate salt of glasdegib. The molecular formula for glasdegib maleate is C25H26N6O5. The molecular weight for glasdegib maleate is 490.51 Daltons. The chemical name of glasdegib maleate is 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate. The molecular structure is shown below:

DAURISMO™ (glasdegib) Structural Formula Illustration

Glasdegib maleate is a white to pale colored powder with pKa values of 1.7 and 6.1. The aqueous solubility of glasdegib maleate is 1.7 mg/mL.

Daurismo (glasdegib) is supplied as a film-coated tablet for oral use containing either 100 mg glasdegib (equivalent to 131.1 mg glasdegib maleate) or 25 mg of glasdegib (equivalent to 32.8 mg glasdegib maleate) together with microcrystalline cellulose, dibasic calcium phosphate anhydrous, sodium starch glycolate, and magnesium stearate as inactive ingredients in the tablet. The film-coating consists of Opadry II® Beige (33G170003) and Opadry II® Yellow (33G120011) containing: hypromellose, titanium dioxide, lactose monohydrate, macrogol, triacetin, iron oxide yellow, and iron oxide red.

INDICATIONS

Daurismo is indicated, in combination with low-dose cytarabine, for the treatment of newly-diagnosed acute myeloid leukemia (AML) in adult patients who are ≥75 years old or who have comorbidities that preclude use of intensive induction chemotherapy.

DOSAGE AND ADMINISTRATION

The recommended dosage of Daurismo is 100 mg orally once daily on days 1 to 28 in combination with cytarabine 20 mg subcutaneously twice daily on days 1 to 10 of each 28-day cycle in the absence of unacceptable toxicity or loss of disease control. For patients without unacceptable toxicity, treat for a minimum of 6 cycles to allow time for clinical response.

Administer Daurismo with or without food. Do not split or crush Daurismo tablets. Administer Daurismo about the same time each day. If a dose of Daurismo is vomited, do not administer a replacement dose; wait until the next scheduled dose is due. If a dose of Daurismo is missed or not taken at the usual time, administer the dose as soon as possible and at least 12 hours prior to the next scheduled dose. Return to the normal schedule the following day. Do not administer 2 doses of Daurismo within 12 hours.

Monitoring And Dosage Modifications

Assess complete blood counts, electrolytes, renal, and hepatic function prior to the initiation of Daurismo and at least once weekly for the first month. Monitor electrolytes and renal function once monthly for the duration of therapy. Obtain serum creatine kinase levels prior to initiating Daurismo and as indicated clinically thereafter (e.g., if muscle symptoms are reported). Monitor electrocardiograms (ECGs) prior to the initiation of Daurismo, approximately one week after initiation, and then once monthly for the next two months to assess for QTc prolongation. Repeat ECG if abnormal. Certain patients may require more frequent and ongoing ECG monitoring [see WARNINGS AND PRECAUTIONS]. Manage any abnormalities promptly [see ADVERSE REACTIONS].

LEAVE A REPLY

Please enter your comment!
Please enter your name here