Octreotide – A Review of its Use in Treating Neuroendocrine Tumours

Abstract

Neuroendocrine tumours (NETs) are a heterogeneous group of neoplasms whose incidence has dramatically increased in recent years. Octreotide is a somatostatin analogue used in the treatment of NETs, and its use in clinical trials has been associated with substantially increased survival. Although traditionally used for the relief of symptoms that result from release of peptides and neuroamines, there has been a growing body of evidence that suggest octreotide has antiproliferative effects. A phase III clinical study has demonstrated that the long-acting formulation (LAR), octreotide LAR, lengthens time to tumour progression in patients with well-differentiated metastatic midgut NETs, and that octreotide LAR is a treatment option for patients with metastatic midgut NETs, regardless of functional status. Furthermore, octreotide LAR has demonstrated clinical efficacy in different types of NETs. These data, along with emerging data on somatostatin analogs, may change the way doctors approach this patient population and reinforce the use of these drugs as a treatment option for patients with non-functioning tumours.

Operative technique in laryngeal paraganglioma: A case series and literature review

“…Octreotide-based therapy has been described in unresectable head and neck paragangliomas and metastatic neuroendocrine tumors of the gastrointestinal and bronchopulmonary tracts. 18,19 It has a role in limiting tumor growth and ameliorating symptoms associated with catecholamine hyper-secretion. However, paragangliomas of the larynx are typically nonsecretory, well localized and amenable to surgical resection via the external cervical approach.…”

“…There is no role for postoperative adjuvant radiotherapy as paragangliomas do not demonstrate malignant behavior. Octreotide‐based therapy has been described in unresectable head and neck paragangliomas and metastatic neuroendocrine tumors of the gastrointestinal and bronchopulmonary tracts 18,19 . It has a role in limiting tumor growth and ameliorating symptoms associated with catecholamine hyper‐secretion.…”

Current treatments and future potential of surufatinib in neuroendocrine tumors (NETs)

“…23 Octreotide is an octapeptide SSA available in a formulation for subcutaneous administration with an action that lasts for 8-12 h. It is also available in a long-acting release form given intramuscularly once every 28 days. 21 Octreotide has high affinity for somatostatin receptors 2 and 5, which are highly expressed in NETs, and works primarily by inhibiting somatostatin-stimulated secretion of hormones and growth factors. In the PROMID study, in patients with advanced well-differentiated midgut NETs, median time to tumor progression was 14.3 months in the octreotide group and 6 months in the placebo group (hazard ratio, 0.34).…”

“…20 Side effects of this class of drugs include GI disturbances and hyperglycemia, and patients may develop gallbladder issues with long-term treatment. 8,21 Significantly, treatment with SSAs results in tumor stabilization in 50% of patients. 22 However, the majority of patients treated with SSAs will go on to experience tumor progression.…”

Synthesis and functionalization of hyperbranched polymers for targeted drug delivery

“…dFCFdWKTCT-ol where dF and dW stand for the D-isomer of phenylalanine and tryptophan and the C-terminus is an alcohol) and somatostatin analog that has a half-life of 1.5 h. Octreotide has been used for targeted neuroendocrine cancer therapy [209,210] due to its high binding affinity to SSTR2 and moderate affinity to SSTR5. [211] Octrotide has been also radiolabeled by complexation with 111 Several EGFR inhibitors have been developed to disrupt the interaction between the EGF and its receptor and show a specific binding ability to tumors.…”