Drug intelligence / Profile preview

etoposide + methylprednisolone + cytarabine + cisplatin + imatinib

Development stage
Phase 2
Lead developer
Bristol Myers Squibb
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen consisting of five drugs: etoposide, methylprednisolone, cytarabine, cisplatin, and imatinib. Etoposide, cytarabine, and cisplatin are chemotherapeutic agents that act by interfering with DNA synthesis or function in rapidly dividing cells. Methylprednisolone is a corticosteroid that exerts anti-inflammatory and immunosuppressive effects and can induce apoptosis in certain cancer cells. Imatinib is a tyrosine kinase inhibitor targeting BCR-ABL as well as other kinases such as c-KIT and PDGFR. This combination would be considered highly experimental; the standard ESHAP regimen (etoposide + methylprednisolone + cytarabine + cisplatin) is used for relapsed or refractory non-Hodgkin lymphoma prior to stem cell transplant[1][2][3][9]. The addition of imatinib may be considered in specific clinical scenarios where BCR-ABL-positive malignancies are present.

02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)DNADNA polymerase familyTOP2A (DNA topoisomerase II)TOP2B (DNA topoisomerase II beta)GR (Glucocorticoid receptor)

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