Drug intelligence / Profile preview

octreotide + tamoxifen

Development stage
Unknown
Lead developer
Novartis
Modality
Peptides, Small Molecules
Administration
Oral, Subcutaneous, Intramuscular, Intravenous
01

Overview

Octreotide + tamoxifen is a combination therapy consisting of two distinct drugs: - **Octreotide** is a synthetic long-acting analog of somatostatin, which inhibits the secretion of several hormones including growth hormone, insulin, and glucagon. It exerts antiproliferative effects on tumor cells by binding to somatostatin receptors (SSTRs) expressed on various tumors. Indirectly, it reduces circulating levels of insulin-like growth factor 1 (IGF-1), which can promote tumor growth. - **Tamoxifen** is a selective estrogen receptor modulator (SERM) that acts as an antagonist at estrogen receptors in breast tissue. It is widely used as hormonal therapy for hormone receptor-positive breast cancer. The rationale for combining these agents stems from preclinical evidence suggesting additive or synergistic antitumor effects through both direct inhibition of tumor cell proliferation and reduction in IGF-1 signaling pathways. This combination has been studied primarily in metastatic breast carcinoma and pancreatic cancer. In clinical trials for metastatic breast cancer, the combination did not show significant improvement over tamoxifen alone in terms of progression-free survival or overall survival but did result in greater reductions in serum IGF-I levels[1][3][4][5]. In small studies involving pancreatic cancer patients, the combination was associated with increased median survival compared to historical controls[2][8].

Other names
octreotide and tamoxifenoctreotide plus tamoxifen
02

Targets

SSTR5 (Somatostatin receptor 5)SSTR2 (Somatostatin receptor type 2)ESR1 (ERα)ESR2 (ERβ)

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