Drug intelligence / Profile preview

idelalisib + rituximab + ifosfamide + carboplatin + etoposide

Development stage
Preclinical
Lead developer
Gilead Sciences
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral (idelalisib; Usually Oral), Intravenous (rituximab, Ifosfamide, Carboplatin, Etoposide)
01

Overview

This regimen is a **combination therapy** that includes five distinct antineoplastic agents: - **Idelalisib**: A small molecule inhibitor targeting phosphatidylinositol 3-kinase delta (PI3Kδ). It induces apoptosis and inhibits proliferation of malignant B-cells, commonly used in certain lymphoid malignancies. - **Rituximab**: A chimeric monoclonal antibody targeting CD20 on B lymphocytes, leading to B-cell depletion[1][3][5]. It is widely used in non-Hodgkin lymphoma, chronic lymphocytic leukemia, and various autoimmune disorders. - **Ifosfamide**: An alkylating agent of the oxazaphosphorine class that inhibits DNA replication and function by forming DNA cross-links. - **Carboplatin**: A platinum compound that causes DNA damage through the formation of intrastrand and interstrand crosslinks, impeding DNA synthesis and function. - **Etoposide**: A podophyllotoxin derivative that inhibits topoisomerase II, thereby causing DNA strand breaks and apoptosis. This multi-agent regimen is investigational as a combination and has only partial preclinical and clinical precedent; combinations such as ICE (ifosfamide, carboplatin, and etoposide) are established for lymphoma and certain solid tumors[2][4][6][8]. Rituximab is routinely added to regimens for B-cell malignancies, while idelalisib is approved for certain refractory lymphoid malignancies. The full five-drug combination is not a standard named protocol.

02

Targets

TOP2A (DNA topoisomerase II)PIK3CD (Phosphatidylinositol 3-kinase delta)CD20 (B-lymphocyte antigen CD20)DNA

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