Drug intelligence / Profile preview

5-fluorouracil + octreotide

Development stage
Preclinical
Lead developer
Novartis
Modality
Small Molecules, MicroRNA (miRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Peptides, Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Recombinant Proteins and Enzymes, Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics
Administration
Intravenous, Subcutaneous
01

Overview

5-fluorouracil + octreotide is a combination of two pharmaceutical agents used primarily in the context of cancer therapy and its complications. 5-fluorouracil (5-FU) is a pyrimidine analog antimetabolite that inhibits thymidylate synthase, thereby interfering with DNA synthesis and exerting cytotoxic effects on rapidly dividing tumor cells[4]. Octreotide is a synthetic somatostatin analogue that inhibits the secretion of various gastrointestinal hormones, reduces intestinal secretions, and slows gastrointestinal motility[2][5]. This combination has been investigated for use in managing severe chemotherapy-induced diarrhea (CID), particularly when caused by regimens containing 5-fluorouracil. Octreotide helps control refractory diarrhea associated with chemotherapy by reducing gut hormone secretion and increasing GI transit time[1][2]. Additionally, both drugs have been studied together for their potential to attenuate local inflammation (by 5-FU) and inhibit autodigestive processes (by octreotide) in conditions such as acute pancreatitis[3].

Other names
continuous 5-fluorouracil infusion plus long-acting octreotidecontinuous5-fluorouracil infusion plus long-acting octreotidecontinuous-5-fluorouracil infusion plus long-acting octreotidemetronomic 5-fluorouracil plus octreotidemetronomic5-fluorouracil plus octreotidemetronomic-5-fluorouracil plus octreotide5-FU + octreotide LAR
02

Targets

SSTR3 (Somatostatin receptor 3)SSTR2 (Somatostatin receptor type 2)SSTR5 (Somatostatin receptor 5)TS (Thymidylate synthase)

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