Dasashil 100mg (Dasatinib)

DESCRIPTION

Dasashil is a second-generation receptor Tyrosine kinase inhibitor. Which binds to Abl with less stringent conformational needed so it exhibits increased effectiveness compared to Imatinib even though with less selectivity. Unlike most RTK inhibitors,
Dasashil linked the active conformation of Bcr-Abl. Is required to treat patients with some Imatinib resistant forms of CML
Dasashil which used as prescription drug under the guidance of doctor.

INDICATION

Dasashil is used for the treatment for Chronic Myeloid Leukaemia: Recently diagnosed adults with Philadelphia chromosome-positive (Ph+) chronic myeloid leukaemia (CML) in chronic phase.

Severe, increased, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib.

Dasashil is used for the treatment for Acute Lymphoblastic Leukaemia: Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukaemia (ALL) with resistance or intolerance to prior therapy

MECHANISM OF ACTION

Dasashil is used for the treatment for Chronic Myeloid Leukaemia: Recently diagnosed adults with Philadelphia chromosome-positive (Ph+) chronic myeloid leukaemia (CML) in chronic phase.

Severe, increased, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib.

Dasashil is used for the treatment for Acute Lymphoblastic Leukaemia: Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukaemia (ALL) with resistance or intolerance to prior therapy

ADME PROPERTY

Plasma protein binding is 96%
volume of distribution 2505 L
Extensively metabolized in humans, mainly by the cytochrome P450 enzyme 3A4.
Dasatinib excreted through the feces.
Half-life is 3-5 hours

DOSAGE MANAGEMENT

• Newly diagnosed: The prescribed dose for Chronic Myeloid Leukaemia is starting 100 mg PO qDay (morning or evening). The drug will be raised to 140 mg qDay if insufficient response.
  • The prescribed dose for Advanced CML is starting 140 mg PO qDay. The drug will increase to 180 mg qDay if insufficient reactions
  • The prescribed dose for Acute Lymphoblastic Leukaemia is starting 140 mg PO qDay. The drug will increase to 180 mg PO qDay if insufficient reactions

PRECAUTION

• When combination with chemotherapy the paediatric patients with Ph+ ALL treated, execute CBCs prior to initial of each block of chemotherapy and as clinically indicated; during consolidation blocks of chemotherapy, do CBCs every 2 days until recovery
• During treatment with Dasashil will causes Myelosuppression includes serious thrombocytopenia, neutropenia and Anemia may develop; may manage by dose interruption, dose reduction, or stopping of treatment; hematopoietic growth factor has been used with resistant myelosuppression.
• Dasashil will occur Hypokalaemia, hypomagnesemia, congenital QT interval prolongation, hepatic impairment
• Use with caution the drug Dasashil in patients who have or may develop prolongation of QT interval

SIDE EFFECTS

• Dyspnea
  • Anorexia
  • Arthralgia
  • Asthenia
  • Constipation
  • Dizziness
  • Musculoskeletal pain
  • Febrile neutropenia
  • Thrombocytopenia
  • Mucosal inflammation
  • Anemia
  • Skin rash
  • Infection
  • Nausea
  • Diarrhea
  • Headache
  • Haemorrhage
  • Fatigue
  • Pyrexia

DRUG INTERACTION

Dasashil concomitant use with CYP3A4 inhibitors will have high Dasatinib plasma concentration.

Dasashil concomitant use with CYP3A4 inducers will lowers Dasatinib plasma concentration.

Dasashil concomitant use with antacids will lower Dasatinib plasma concentration.

Dasashil concomitant use with H2 antagonists/proton pump inhibitors will lowers Dasatinib plasma concentration.

Dasashil concomitant use with CYP3A4 substrates will have their plasma concentration changed by Dasatinib.

PREGNANCY

Pregnancy category D: Dasashil will resulted in fetal harm during pregnancy. Discuss with pregnant woman of the possible risk to a foetus.

LACTATION

Avoid breast feeding during Dasashil treatment.

STORAGE

Stored at 20°C – 25°C

MISSED DOSE

If missed dose occurs, patients must consult with medical oncologist and follow the regular dosing schedule.