Lanreotide Depot: An Antineoplastic Treatment of Carcinoid or Neuroendocrine Tumors

Abstract

PurposePeptide drugs for antineoplastic therapies usually have low oral bioavailability and short in vivo half-lives, requiring less preferred delivery methods. Lanreotide depot is a sustained-release somatostatin analog (SSA) formulation produced via an innovative peptide self-assembly method. Lanreotide is approved in the USA and Europe to improve progression-free survival (PFS) in patients with unresectable gastroenteropancreatic neuroendocrine tumors (GEP-NETs) and also approved in Europe for symptom control in carcinoid syndrome associated with GEP-NETs. This review discusses how the distinct molecule and formulation of lanreotide depot provide advantages to patients and health care providers, as well as the most recent clinical evidence demonstrating the safety and efficacy of lanreotide depot in inhibiting tumor growth and controlling hormonal symptoms in GEP-NETs.Methodology and ResultsThe lanreotide depot formulation confers a remarkable pharmacokinetic profile with no excipients, comprised only of lanreotide acetate and water. Of note, lanreotide depot constitutes an example for peptide self-assembly based formulations, providing insights that could help future development of sustained-release formulations of other antineoplastic peptides. Most patients with GEP-NETs will present with inoperable or incurable disease; thus, medical management for symptoms and tumor control plays a crucial role. Recent long-term clinical studies have demonstrated that lanreotide depot is well tolerated, prolongs PFS in GEP-NET patients, and significantly reduces symptoms related to carcinoid syndrome.ConclusionsThe unique depot formulation and delivery method of lanreotide confer advantages in the treatment of metastatic GEP-NETs, contributing to improvements in NET-related symptoms and PFS without reducing quality of life in this patient population.

Structural Characterization of PEGylated Hexaphenylalanine Nanostructures Exhibiting Green Photoluminescence Emission

“…The ability of peptides to self‐assemble, adopting stable secondary conformations, has allowed them to be used in nanotechnology and in materials science as very multifunctional tools . Superhydrophobic coating, tissue engineering, cell culturing, biosensing, and drug delivery are only some of the possible areas of application of peptide‐based supramolecular systems. The driving forces that hold up spontaneous aggregations are pinpointed in hydrogen bonds and hydrophobic and aromatic interactions.…”

Selective internal radiation therapy: an effective treatment for hormonal syndromes in pancreatic neuroendocrine tumors

“…However, symptoms may not be fully or persistently controlled despite optimal SSA therapy, due to an as of yet unresolved escape phenomenon [18]. SSA induce an important symptomatic improvement in most of the cases (70%), [19] but patients usually become refractory to this therapy because of the development of desensitization [20] months after the beginning of the treatment [21].…”

Preoperative and long-term efficacy and safety of lanreotide autogel in patients with thyrotropin-secreting pituitary adenoma: a multicenter, single-arm, phase 3 study in Japan

“…In most TSHomas, the tumor cells are strongly positive for SSTR2 [16,17]. Two formulations of lanreotide have been used to treat TSHoma [4]: lanreotide prolonged release (LAN-PR, Somatuline ® LA) for intramuscular injection every 7 to 14 days [18], and lanreotide autogel (LAN-ATG, Somatuline ® Autogel ® ), which is a sustained-release, supersaturated formulation of the lanreotide and is supplied in ready-to-use, prefilled syringes, for deep subcutaneous injection every 4 weeks [19,20]. The use of LAN-PR for TSHoma has been approved in 17 countries [18] based on a clinical trial conducted in Europe [8].…”