Drug intelligence / Profile preview

gemcitabine + epirubicin

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Intravenous
01

Overview

Gemcitabine + epirubicin is a combination chemotherapy regimen comprising two distinct small molecule cytotoxic agents: **gemcitabine**, a nucleoside analog (antimetabolite), and **epirubicin**, an anthracycline antibiotic. - **Gemcitabine** inhibits DNA synthesis by incorporation into replicating DNA, causing chain termination and subsequent apoptosis; it also inhibits ribonucleotide reductase, further depleting deoxynucleotide pools required for DNA replication. - **Epirubicin** intercalates into DNA and inhibits topoisomerase II, leading to DNA strand breaks and inhibition of cell division. Combined administration produces additive or potentially synergistic effects on tumor cell cytotoxicity, including induction of DNA breaks not easily repaired, enhancing apoptotic signals. Primarily investigated for use in advanced and metastatic breast cancer and advanced pancreatic cancer, the combination has demonstrated activity as first-line chemotherapy and is generally well-tolerated with hematologic toxicity (mainly neutropenia) as the dose-limiting side effect. The combination is evaluated in phase II clinical trials and is sometimes used in multi-agent regimens (e.g., with taxanes such as paclitaxel), but gemcitabine + epirubicin together (without another agent) is a distinct regimen as well[4][8].

Brand names
GemzarEllence
Other names
gemcitabine hydrochlorideepirubicin hydrochloride
02

Targets

DNA polymerase familyRNR (Ribonucleotide reductase)DNATOP2A (DNA topoisomerase II)

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