DDInter224 DDInter1435
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
Pexidartinib is a selective tyrosine kinase inhibitor that works by inhibiting the colony-stimulating factor (CSF1)/CSF1 receptor pathway. Pexidartinib was originally developed by Daiichi Sankyo, Inc. and it was approved by the FDA in August 2019 as the first systemic therapy for adult patients with symptomatic tenosynovial giant cell tumor. Tenosynovial giant cell tumor is a rare form of non-malignant tumor that causes the synovium and tendon sheaths to thicken and overgrow, leading to damage in surrounding joint tissue.[A182240,L7901] Debilitating symptoms often follow with tenosynovial giant cell tumors, along with a risk of significant functional limitations and a reduced quality of life in patients. While surgical resection is a current standard of care for tenosynovial giant cell tumor, there are tumor types where surgeries are deemed clinically ineffective with a high risk of lifetime recurrence. Pexidartinib works by blocking the immune responses that are activated in tenosynovial giant cell tumors. In clinical trials, pexidartinib was shown to promote improvements in patient symptoms and functional outcomes in TGCT. Pexidartinib is available in oral formulations and it is commonly marketed as Turalio.
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