DDInter224 DDInter899
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.[A6902,A261796,A261801] 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.[A6901,A17961] Bosutinib was first approved by the FDA in
Ibrutinib is a small molecule that acts as an irreversible potent inhibitor of Burton's tyrosine kinase. It is designated as a targeted covalent drug and presented as a promising activity in B-cell malignancies in clinical trials. Ibrutinib was developed by Pharmacyclics Inc and was first approved by the FDA in November 2013 for the treatment of mantle cell lymphoma (MCL) under accelerated approval; however, in April 2023, the drug manufacturer withdrew the accelerated approvals for ibrutinib in the US. Ibrutinib was approved by the EMA in October 2014 and by Health Canada in November 2014. It is currently approved for the treatment of various conditions, such as chronic lymphocytic leukemia (CLL), Waldenström's Macroglobulinemia, and chronic graft versus host disease (cGVHD) in August 2017. Notably, ibrutinib became the first FDA-approved cGVHD treatment for children in August 2017.
Bosutinib {u} (Compound) resembles {v} (Compound) Gefitinib
Bosutinib {u} (Compound) binds {v} (Gene) PTK2
Bosutinib {u} (Compound) upregulates {v} (Gene) HSD17B7
Bosutinib {u} (Compound) is included by {v} (Pharmacologic Class) P-Glycoprotein Inhibitors
Bosutinib {u} (Compound) downregulates {v} (Gene) COTL1
Bosutinib {u} (Compound) causes {v} (Side Effect) Cardiac disorder
Bosutinib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Metronidazole
Bosutinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Famotidine
Bosutinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Magnesium carbonate
Bosutinib {u} may lead to a major life threatening interaction when taken with {v} Mumps virus strain B level jeryl lynn live antigen
Bosutinib (Compound) resembles Gefitinib (Compound)
Bosutinib (Compound) binds PTK2 (Gene)
Bosutinib (Compound) upregulates HSD17B7 (Gene)
Bosutinib (Compound) is included by P-Glycoprotein Inhibitors (Pharmacologic Class)
Bosutinib (Compound) downregulates COTL1 (Gene)
Bosutinib (Compound) causes Cardiac disorder (Side Effect)
Bosutinib may cause a minor interaction that can limit clinical effects when taken with Metronidazole
Bosutinib may cause a moderate interaction that could exacerbate diseases when taken with Famotidine
Bosutinib may cause a moderate interaction that could exacerbate diseases when taken with Magnesium carbonate
Bosutinib may lead to a major life threatening interaction when taken with Mumps virus strain B level jeryl lynn live antigen