SOMATOSTATIN ANALOGUES FOR THE TREATMENT OF NEUROENDOCRINE TUMOURS. DOSAGE FORMS AND ROUTES OF ADMINISTRATION (REVIEW)
DOI:
https://doi.org/10.22159/ijap.2020v12i2.36558Keywords:
Neuroendocrine tumours, Somatostatin analogues, Dosage form of prolonged-release, Oral administrationAbstract
This review summarises information on drug products Somatostatin Analogues (SSAs), which are included in the algorithm of Neuroendocrine Tumors (NET) treatment. SSAs are the current standard for safe and effective management of NET symptoms and control of tumours growth and are administered in a range of dosage forms for parenteral administration, such as intramuscular, subcutaneous and implant. A search criterion was the therapy of NET with medicines from a group of SSAs. Literature survey has been done in a range of years 1990-2018 to make the review updated and comprehensive and to show the development of SSAs new pharmaceutical dosage forms to improve patient quality of life and side effects decrease. The sources were world-recognized journals. Keywords used as filters were NET, SSAs, octreotide, lanreotide, pasireotide, Somatostatin Receptors (SSTR), dosage form. The current review is created with an intended to focus on the advantage of SSAs modern dosage forms. Literature survey revealed that many studies were carried out to SSAs encapsulation into microspheres that changes the drug bioavailability and allows reducing the number of administration. Also, SSAs delivery systems in particular devices such as auto-injector have been created to control the continuous concentration of the drug and to provide safety guarantee. Besides, studies have been carried out to prepare SSAs formulations for oral administration to improve the quality of life of the NET patients. In this review, SSAs pharmaceutical dosage forms with improved pharmacokinetic and therapeutic characteristics and routes of administration are analyzed.
Downloads
References
Fraenkel M, Fagiano A, Valk GD. Epidemiology of neuroendocrine tumors. Front Horm Res 2015;44:1-23.
Jimenez Fonseca P, Carmona Bayonas A, Martin Perez E, Crespo G, Serrano R, Llanos M, et al. Health-related quality of life in well-differentiated metastatic gastroenteropancreatic neuroendocrine tumors. Cancer Metastasis Rev 2015;3:381-400.
Chalabi M, Duluc C, Caron P, Vezzosi D, Guillermet Guibert J, Pyronnet St, et al. Somatostatin analogs: does pharmacology impact antitumor efficacy? Trends Endocrinol Metab 2014;3:115-27.
Narayanan S, Kunz PL. Role of somatostatin analogues in the treatment of neuroendocrine tumors. Hematol Oncol Clin North Am 2016;1:163-77.
Mazziotti G, Mosca A, Frara S, Vitale G, Giustina A. Somatostatin analogs in the treatment of neuroendocrine tumors: current and emerging aspects. Expert Opin Pharmacother 2017;16:1679-89.
Grozinsky Glasberg S, Shimon I, Korbonits M, Grossman AB. Somatostatin analogues in the control of neuroendocrine tumours: efficacy and mechanisms. Endocr Relat Cancer 2008;3:701-20.
Anthony L, Freda PU. From somatostatin to octreotide LAR: evolution of a somatostatin analogue. Curr Med Res Opin 2009;12:2989-99.
Katznelson L, Atkinson JL, Cook DM, Ezzat SZ, Hamrahian AH, Miller KK. American association of clinical endocrinologists medical guidelines for clinical practice for the diagnosis and treatment of acromegaly-2011 update executive summary. Endocr Pract 2011;17 Suppl 4:1-44.
Patel D, Chan D, Cenic G, Pavlakis N, Proce TJ. Systemic therapies for advanced gastroenteropancreatic neuroendocrine tumors. Expert Rev Endocrinol Metab 2016;4:311-27.
Kunz PL, Reidy Lagunes D, Anthony LB, Bertino EM, Brendtro K, Chan JA, et al. Consensus guidelines for the management and treatment of neuroendocrine tumors. Pancreas 2013;4:557-77.
Oberg KE. The management of neuroendocrine tumours: current and future medical therapy options. Clin Oncol 2012;4:282-93.
Rai U, Thrimawithana TR, Valery C, Young SA. Therapeutic uses of somatostatin and its analogues: current view and potential applications. Pharmacol Ther 2015;152:98-110.
Bousquet C, Lasfargues C, Chalabi M, Billah SM, Susini C, Vezzosi D, et al. Current scientific rationale for the use of somatostatin analogs and mTOR inhibitors in neuroendocrine tumor therapy. J Clin Endocrinol Metab 2012;3:727-37.
Massironi S, Zilli A, Conte D. Somatostatin analogs for gastric carcinoids: for many, but not all. World J Gastroenterol 2015;22:6785-93.
Mohammed GK, Obaidat RM, Assaf S, Khanfar M, Al-taani B. Formulations and technologies in growth hormone delivery. Int J Pharm Pharm 2017;7:1-12.
Wolin EM. The expanding role of somatostatin analogs in the management of neuroendocrine tumors. Gastrointest Cancer Res 2012;5:161-8.
Crabtree JS. Clinical and preclinical advances in gastroenteropancreatic neuroendocrine tumor therapy. Front Endocrinol 2017;8:341.
Ruscica M, Arvigo M, Steffani L, Ferone D, Magni P. Somatostatin, somatostatin analogs and somatostatin receptor dynamics in the biology of cancer progression. Curr Mol Med 2013;4:555-71.
Rubin J, Ajani J, Schirmer W, Venook AP, Bukowski R, Pommier R, et al. Octreotide acetate long-acting formulation versus open-label subcutaneous octreotide acetate in malignant carcinoid syndrome. J Clin Oncol 1999;2:600-6.
Tiberg F, Johnsson M, Jankunec M, Barauskas J. Phase behavior, functions, and medical applications of soy phosphatidylcholine and diglyceride lipid compositions. Chem Lett 2012;10:1090-2.
Tiberg F, Johnsson M. Drug delivery applications of non-lamellar liquid crystalline phases and nanoparticles. J Drug Delivery Sci Technol 2011;1:101-9.
Tiberg F, Roberts J, Cervin C, Johnsson M, Sarp S, Tripanti AP, et al. Octreotide s. c. depot provides sustained octreotide bioavailability and similar IGF-1 suppression to octreotide LAR in healthy volunteers. Br J Clin Pharmacol 2015;3:460-72.
Tekade RK. editor. Biomaterials and bionanotechnology (Advances in pharmaceutical product. Development and research series) 1st ed. Ahmedabad: Academic Press (Elsevier); 2019.
Chieffo C, Cook D, Xiang Q, Frohman LA. Efficacy and safety of an octreotide implant in the treatment of patients with acromegaly. J Clin Endocrinol Metab 2013;10:4047-54.
Gadelha MR, Chieffo C, Bai SA, Hu X, Frohman LA. A subcutaneous octreotide hydrogel implant for the treatment of acromegaly. Endocr Pract 2012;6:870-81.
Hofland LJ, Van der Hoek J, Feelders R, van der Lely AJ, de Herder W, Lamberts SW. Pre-clinical and clinical experiences with novel somatostatin ligands: advantages, disadvantages and new prospects. J Endocrinol Invest 2005;28(11 Suppl):36-42.
Lombardi G, Minuto F, Tamburrano G, Ambrosio MR, Arnaldi G, Arosio M, et al. Efficacy of the new long-acting formulation of lanreotide (lanreotide Autogel) in somatostatin analog-naive patients with acromegaly. J Endocrinol Invest 2009;3:297-303.
Siepmann J, Faisant N, Akiki J, Richard J, Benoit JP. Effect of the size of biodegradable microparticles on drug release: experiment and theory. J Controlled Release 2004;1:123-34.
Estey T, Kang J, Schwendeman SP, Carpenter JF. BSA degradation under acidic conditions: a model for protein instability during release from PLGA delivery systems. J Pharm Sci 2006;7:1626-39.
Lewis AL, Illum L. Formulation strategies for sustained release of proteins. Ther Delivery 2010;3:457-79.
Gobeaux F, Fay N, Tarabout C, Meriadec C, Meneau F, Ligeti M, et al. Structural role of counterions adsorbed on self-assembled peptide nanotubes. J Am Chem Soc 2012;1:723-33.
Gobeaux F, Fay N, Tarabout C, Meneau F, Meriadec C, Delvaux C, et al. Experimental observation of double-walled peptide nanotubes and monodispersity modeling of the number of walls. Langmuir 2013;8:2739-45.
Pandit A, Fay N, Bordes L, Valery C, Cherif Cheikh R, Robert B, et al. Self-assembly of the octapeptide lanreotide and lanreotide-based derivatives: the role of the aromatic residues. J Pept Sci 2008;1:66-75.
Pouget E, Dujardin E, Cavalier A, Moreac A, Valery C, Marchi Artzner V, et al. Hierarchical architectures by the synergy between dynamical template self-assembly and biomineralization. Nat Mater 2007;6:434-9.
Pouget E, Fay N, Dujardin E, Jamin N, Berthault P, Perrin L, et al. Elucidation of the self-assembly pathway of lanreotide octapeptide into beta-sheet nanotubes: role of two stable intermediates. J Am Chem Soc 2010;12:4230-41.
Valery C, Artzner F, Robert B, Gulick T, Keller G, Grabielle Madelmont C, et al. Self-association process of a peptide in solution: from beta-sheet filaments to large embedded nanotubes. Biophys J 2004;4:2484-501.
Valery C, Pouget E, Pandit A, Verbavatz JM, Bordes L, Boisde I, et al. Molecular origin of the self-assembly of lanreotide into nanotubes: a mutational approach. Biophys J 2008;5:1782-95.
Gobeaux F, Fay N, Tarabout C, Meriadec C, Meneau F, Ligeti M, et al. Structural role of counterions adsorbed on self-assembled peptide nanotubes. J Am Chem Soc 2012;1:723-33.
Troconiz IF, Cendros JM, Peraire C, Ramis J, Garrido MJ, Boscani PF, et al. Population pharmacokinetic analysis of lanreotide autogel in healthy subjects: evidence for injection interval of up to 2 mo. Clin Pharmacokinet 2009;1:51-62.
Buil Bruna N, Garrido M, Dehez M, Manon A, Nguyen THQ, Gomez Panzani El, et al. Population pharmacokinetic analysis of lanreotide autogel (®)/Depot in the treatment of neuroendocrine tumors: pooled analysis of four clinical trials. Clin Pharmacokinet 2016;4:461-73.
Adelman DT, Burgess A, Davies PR. Evaluation of long-acting somatostatin analog injection devices by nurses: a quantitative study. Med Devices (Auckl) 2012;5:103-9.
Witek P, Mucha S, Ruchata M. Patient satisfaction and preferences of lanreotide autogel treatment in acromegaly. Endokrynol Pol 2016;6:572-9.
Wolin EM, Manon A, Chassaing C, Lewis A, Bertocchi L, Richard J, et al. Lanreotide depot: an antineoplastic treatment of carcinoid or neuroendocrine tumors. J Gastrointest Cancer 2016;4:366-74.
Susini C, Buscail L. Rationale for the use of somatostatin analogs as antitumor agents. Ann Oncol 2006;12:1733-42.
Oberg K, Kvols LK, Caplin M, Delle Fave G, de Herder W, Rindi G, et al. Consensus report on the use of somatostatin analogs for the management of neuroendocrine tumors of the gastroenteropancreatic system. Ann Oncol 2004;6:966-73.
Bruns C, Lewis I, Briner U, Meno Tetang G, Weckbecker G. SOM230: a novel somatostatin peptidomimetic with broad somatotropin release inhibiting factor (SRIF) receptor binding and a unique antisecretory profile. Eur J Endocrinol 2002;5:707-16.
Schmid HA. Pasireotide (SOM230): development, mechanism of action and potential applications. Mol Cell Endocrinol 2008;1-2:69-74.
Golor G, Hu K, Ruffin M, Buchelt A, Bouillaud E, Wang Y, et al. A first-in-man study to evaluate the safety, tolerability, and pharmacokinetics of pasireotide (SOM230), a multireceptor-targeted somatostatin analog, in healthy volunteers. Drug Des Dev Ther 2012;6:71-9.
Petersenn S, Schopohl J, Barkan A, Mohideen P, Colao A, Abs R, et al. Pasireotide (SOM230) demonstrates efficacy and safety in patients with acromegaly: a randomized, multicenter, phase II trial. J Clin Endocrinol Metab 2010;6:2781-9.
Feelders RA, de Bruin C, Pereira AM, Romijn JA, Netea Maier RT, Hermus AR, et al. Pasireotide alone or with cabergoline and ketoconazole in cushing’s disease. N Engl J Med 2010;19:1846-8.
Boscaro M, Ludlam WH, Atkinson B, Glusman JE, Petersenn S, Reincke M, et al. Treatment of pituitary-dependent cushing’s disease with the multireceptor ligand somatostatin analog pasireotide (SOM230): a multicenter, phase II trial. J Clin Endocrinol Metab 2009;1:115-22.
Kohli S, Pal A, Jain S. Preparation, characterization and evaluation of poly(lactide-co-glycolide) microspheres for the controlled release of zidovudine. Int J Pharm Pharm 2017;12:70-7.
Settu K, Vaiyapuri M. Formulation and evaluation of isorhamnetin loaded poly lactic-co-glycolic acid nanoparticles. Asian J Pharm Clin Res 2017;11:177-81.
El-feky GS, Zayed GM. PLGA nanoparticles loaded mucoadhesive and termosensitive hydrogel as potential platform for the treatment of oral mucositis. Int J Appl Pharm 2019;1:106-12.
Mishra R, Mir SR, Amin S. Polymeric nanoparticles for improved bioavailability of cilnidipine. Int J Pharm Pharm 2017;4:129-33.
Cuevas Ramos D, Fleseriu M. Pasireotide: a novel treatment for patients with acromegaly. Drug Des Dev Ther 2016;10:227-39.
Kvols LK, Oberg KE, O’Dorisio TM, Mohideen P, De Herder WW, Arnold R, et al. Pasireotide (SOM230) shows efficacy and tolerability in the treatment of patients with advanced neuroendocrine tumors refractory or resistant to octreotide LAR: results from a phase II study. Endocr Relat Cancer 2012;5:657-66.
Norman P. Vapreotide (Debipharm). I Drugs 2000;11:1358-72.
Dasgupta P, Mukherjee R. Lipophilization of somatostatin analog RC-160 with long chain fatty acid improves its antiproliferative and antiangiogenic activity in vitro. Br J Pharmacol 2000;1:101-9.
Vapreotide (BMY 41606, RC 160, Sanvar®). Drugs in R and D 2003;5:326-30.
Shaji J, Patole V. Protein and peptide drug delivery: oral approaches. Indian J Pharm Sci 2008;3:269-77.
Bak A, Leung D, Barrett SE, Forster S, Minnihan EC, Leithead AW, et al. Physicochemical and formulation developability assessment for therapeutic peptide delivery-a primer. AAPS J 2015;1:144-55.
Thundimadathil J. Cancer treatment using peptides: current therapies and future prospects. J Amino Acids 2012. Doi:10.1155/2012/967347
Preet P. Peptides: a new therapeutic approach. Int J Curr Pharm Res 2018;2:29-34.
Dorkoosh FA, Verhoef JC, Verheijden JH, Rafiee Tehrani M, Borchard G, Junginger HE. Peroral absorption of octreotide in pigs formulated in delivery systems on the basis of superporous hydrogel polymers. Pharm Res 2002;10:1532-6.
Thanou M, Verhoef JC, Marbach P, Junginger HE. Intestinal absorption of octreotide: N-trimethyl chitosan chloride (TMC) ameliorates the permeability and absorption properties of the somatostatin analogue in vitro and in vivo. J Pharm Sci 2000;7:951-7.
Thanou M, Verhoef JC, Verheijden JH, Junginger HE. Intestinal absorption of octreotide using trimethyl chitosan chloride: studies in pigs. Pharm Res 2001;6:823-8.
McCartney F, Gleeson JP, David J, Brayden DJ. Safety concerns over the use of intestinal permeation enhancers: a mini-review. Tissue Barriers 2016;2:e1176822.
Tuvia S, Salama P, Weinstein I, Marom K, Neumark E, Arama ML, et al. Octreolin a safe oral alternative for parenteral octreotide treatment. Growth Horm IGF Res 2010;20 Suppl 1:835-6.
Tuvia S, Atsmon J, Teichman SL, Katz S, Salama P, Pelled D, et al. Oral octreotide absorption in human subjects: comparable pharmacokinetics to parenteral octreotide and effective growth hormone suppression. J Clin Endocrinol Metab 2012;7:2362-9.
Melmed S, Popovic V, Bidlingmaier M, Mercado M, Van Der Lely AJ, Biermasz N, et al. Safety and efficacy of oral octreotide in acromegaly: results of a multicenter phase III trial. J Clin Endocrinol Metab 2015;4:1699-708.
Maggio ET, Grasso P. Oral delivery of octreotide acetate in Intravail® improves uptake, half-life, and bioavailability over subcutaneous administration in male swiss webster mice. Regul Pept 2011;2-3:233-8.
Osipov VN, Sushinina LP, Ustinkina SV, Smirnova LI, Shprakh ZS. Cyphetrylin cytotoxic analogues (report I). Russ J Biother 2016;4:85-8.
Borisova LM, Kiseleva MP, Osipov VN, Sushinina LP, Ustinkina SV, Smirnova LI, et al. Cyphetrylin cytotoxic analogues (report II). Russ J Biother 2017;2:23-9.
Shprakh ZS, Yartseva IV, Ignateva EV, Smirnova AP, Sushinina LP, Ustinkina SV, et al. Synthesis and chemico-pharmaceutical characteristics of somatostatin analog with antitumor activity. Pharm Chem J 2014;3:159-62.
Mikhaevich ЕI, Yavorskaya NP, Golubeva IS, Polozkova AP, Partolina SA, Oborotova NA. Studying the possibility of oral delivery of cyphetrylin. Russ J Biother 2012;1:3-7.
Shprakh ZS, Ignаtieva ЕV, Yartseva IV, Dmitricheva NA, Smirnova LI. Development and validation of cyphetrylin assay in tablets. Russ J Biother 2016;3:55-61.
Shprakh ZS, Borisova LM, Kiseleva MP, Smirnova ZS. Preclinical study of cyphetrylin antitumor efficiency on experimental animal tumors. Exp Clin Pharmacol 2019;8:27-31.
Zimakova NI, Kolesnikova EY, Budko AP, Deychman ZG, Zolotarev AE, Badun GA, et al. Preclinical study pharmacokinetics drug form of analog hypothalamic hormone somatostatine (AGG). Russ J Biother 2012;3:33-8.
Konyaeva OI, Kulbachevskaya NYu, Ermakova NP, Chaley VA, Merkulova IB, Abramova ТV, et al. Pre-clinical toxicological study of analogue of hypothalamic hormone. Russ J Biother 2018;2:63-70.
Published
How to Cite
Issue
Section
