Drug intelligence / Profile preview

everolimus + pasireotide LAR

Development stage
Phase 2
Lead developer
Novartis
Modality
Small Molecules, Peptides
Administration
Oral, Intramuscular
01

Overview

A combination therapy comprising **everolimus**, an oral mTOR (mechanistic target of rapamycin) inhibitor, and **pasireotide LAR** (long-acting release), a second-generation somatostatin analog. Everolimus inhibits the mTOR signaling pathway, reducing cellular proliferation and tumor growth mainly through inactivation of mTORC1, leading to reduced phosphorylation of S6 kinase and 4E-BP1. Pasireotide LAR targets multiple somatostatin receptor subtypes (including sstr1, 2, 3, and 5), suppressing growth hormone secretion and reducing levels of insulin-like growth factor-1 (IGF-1), as well as exerting direct antiproliferative effects on neuroendocrine tumors. The combination is primarily investigated for the treatment of advanced, well-differentiated, progressive pancreatic and gastrointestinal neuroendocrine tumors, aiming to achieve dual antiproliferative and antisecretory effects.

Other names
everolimus + pasireotide LAR
02

Targets

HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))CYP2D6 (Cytochrome P450 2D6)CYP3A (CYP3A family)FKBP1AGHSR (Growth hormone secretagogue receptor)KOR (Kappa opioid receptor)SSTR1 (Somatostatin Receptor Type 1)SSTR2 (Somatostatin receptor type 2)SSTR3 (Somatostatin receptor 3)SSTR5 (Somatostatin receptor 5)Mechanistic target of rapamycin complex 1

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