GastrointestinalFDA Approved

Pasireotide (Signifor)

Subcutaneous injection (twice daily), Intramuscular injection (monthly LAR)

Overview

A multireceptor-targeted somatostatin analog with high binding affinity for SSTR1, SSTR2, SSTR3, and SSTR5, particularly notable for its 40-fold greater affinity for SSTR5 compared to octreotide. This receptor profile makes pasireotide uniquely effective in Cushing's disease, where corticotroph adenomas predominantly express SSTR5.

Mechanism of Action

Pasireotide suppresses ACTH secretion from pituitary corticotroph tumors, reducing cortisol production..

Research Summary & Key Findings

FDA-approved for Cushing's disease (2012) and acromegaly (LAR formulation, 2014). Phase III trial in Cushing's disease demonstrated normalization of urinary free cortisol in 26% of patients at 6 months (Colao et al., NEJM, 2012). Superior efficacy to octreotide LAR in acromegaly patients not controlled on first-generation somatostatin analogs. Hyperglycemia is the most significant side effect due to SSTR5-mediated insulin suppression.

Clinical Status

FDA Approved

Pasireotide (Signifor) has received FDA approval and is available for clinical use under appropriate medical supervision. Consult a qualified healthcare provider for prescribing information.

Administration Routes

Subcutaneous injection (twice daily)Intramuscular injection (monthly LAR)

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Disclaimer: This information is provided for educational and research purposes only. It is not intended as medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before starting any peptide therapy. The Peptide Association does not endorse or recommend any specific treatment protocol.