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Bosutinib

Generic Name
Bosutinib
Brand Names
Bosulif
Drug Type
Small Molecule
Chemical Formula
C26H29Cl2N5O3
CAS Number
380843-75-4
Unique Ingredient Identifier
5018V4AEZ0

Overview

Bosutinib is a 7-alkoxy-3-quinolinecarbonitrile that functions as a potent, dual SRC and ABL tyrosine kinase inhibitor indicated for chronic myelogenous leukemia (CML), specifically Philadelphia chromosome-positive (Ph+) CML. Philadelphia chromosome is a hallmark of CML due to the reciprocal translocation t(9;22)(q34;q11), resulting in a BCR-ABL fusion protein. The first BCR-ABL inhibitor, imatinib, was introduced over a decade ago as a breakthrough in CML management; however, emerging resistance to imatinib poses challenges in achieving remission. Second-generation BCR-ABL inhibitors like bosutinib inhibit most resistance-conferring BCR-ABL mutations except V299L and T315, thus providing more therapeutic options for patients. Bosutinib was first approved by the FDA in 2012 for the treatment of adult chronic, accelerated, or blast-phase Ph+ CML with resistance or intolerance to prior therapy. On September 26, 2023, bosutinib was also approved by the FDA for the treatment of pediatric CML that is newly diagnosed or resistant/intolerant to prior therapy. This approval was based on favorable results obtained from the open-label, randomized, multicenter trial BFORE that showed a significant improvement in major molecular response, defined as a ≤0.1% BCR ABL ratio on an international scale, with bosutinib treatment.

Background

Bosutinib is a 7-alkoxy-3-quinolinecarbonitrile that functions as a potent, dual SRC and ABL tyrosine kinase inhibitor indicated for chronic myelogenous leukemia (CML), specifically Philadelphia chromosome-positive (Ph+) CML. Philadelphia chromosome is a hallmark of CML due to the reciprocal translocation t(9;22)(q34;q11), resulting in a BCR-ABL fusion protein. The first BCR-ABL inhibitor, imatinib, was introduced over a decade ago as a breakthrough in CML management; however, emerging resistance to imatinib poses challenges in achieving remission. Second-generation BCR-ABL inhibitors like bosutinib inhibit most resistance-conferring BCR-ABL mutations except V299L and T315, thus providing more therapeutic options for patients. Bosutinib was first approved by the FDA in 2012 for the treatment of adult chronic, accelerated, or blast-phase Ph+ CML with resistance or intolerance to prior therapy. On September 26, 2023, bosutinib was also approved by the FDA for the treatment of pediatric CML that is newly diagnosed or resistant/intolerant to prior therapy. This approval was based on favorable results obtained from the open-label, randomized, multicenter trial BFORE that showed a significant improvement in major molecular response, defined as a ≤0.1% BCR ABL ratio on an international scale, with bosutinib treatment.

Indication

用于治疗对既往治疗无效的慢性、加速期或急变期Ph+的慢性粒细胞白血病(CML)患者。

Associated Conditions

  • Accelerated Phase Chronic Myelogenous Leukemia (CML)
  • Chronic Phase Chronic Myeloid Leukemia
  • Blast phase Chronic myeloid leukemia

Clinical Trials

Title
Posted
Study ID
Phase
Status
Sponsor
2024/05/21
Phase 3
Recruiting
2024/03/07
N/A
Not yet recruiting
2022/05/06
N/A
Completed
2022/03/18
N/A
Completed
2021/09/02
Phase 1
Completed
2021/07/21
Phase 3
Active, not recruiting
2021/06/08
Phase 1
Completed
2021/05/07
Phase 4
Recruiting
2021/03/11
Phase 1
Terminated
Fundacion Espanola para la Curacion de la Leucemia Mieloide Cronica
2021/02/09
Phase 1
Recruiting

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
Pfizer Laboratories Div Pfizer Inc
0069-0136
ORAL
500 mg in 1 1
9/29/2023
Pfizer Laboratories Div Pfizer Inc
0069-0504
ORAL
50 mg in 1 1
9/29/2023
U.S. Pharmaceuticals
63539-117
ORAL
100 mg in 1 1
10/28/2021
Pfizer Laboratories Div Pfizer Inc
0069-0193
ORAL
400 mg in 1 1
9/29/2023
U.S. Pharmaceuticals
63539-193
ORAL
400 mg in 1 1
10/28/2021
Pfizer Laboratories Div Pfizer Inc
0069-0135
ORAL
100 mg in 1 1
9/29/2023
Pfizer Laboratories Div Pfizer Inc
0069-1014
ORAL
100 mg in 1 1
9/29/2023

EMA Drug Approvals

Approved Product
Authorization Holder
Status
Issued Date
No EMA approvals found for this drug.

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
No HSA approvals found for this drug.

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

Approved Product
ARTG ID
Sponsor
Registration Type
Status
Registration Date
BOSULIF bosutinib 100 mg tablet blister pack
208809
Medicine
A
4/29/2014
BOSULIF bosutinib 500 mg tablet blister pack
208810
Medicine
A
4/29/2014
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