Review




Structured Review

Ipsen Group somatuline depot
On the top is the sequence of the native somatostatin peptide. The blue sequence in somatostatin represents a key pharmacophore in somatostatin, responsible for receptor binding. In somatostatin analogues, lysine (K) is conserved, while tryptophan is replaced with its stereoisomers in octreotide, <t>lanreotide,</t> vapreotide, and pasireotide. Phenylalanine is substituted with tyrosine, which has an additional hydroxyl group, and threonine is replaced with a more hydrophobic amino acid, such as valine, in lanreotide and vapreotide. Pasireotide incorporates the highest number of unnatural amino acids. In this analogue, cyclization occurs between the N- and C-terminal ends, while in octreotide, lanreotide, and vapreotide, cyclization involves the side chains of cysteine residues, similar to native somatostatin.
Somatuline Depot, supplied by Ipsen Group, used in various techniques. Bioz Stars score: 86/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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Images

1) Product Images from "Advances in Peptidomimetics for Next-Generation Therapeutics: Strategies, Modifications, and Applications"

Article Title: Advances in Peptidomimetics for Next-Generation Therapeutics: Strategies, Modifications, and Applications

Journal: Chemical Reviews

doi: 10.1021/acs.chemrev.4c00989

On the top is the sequence of the native somatostatin peptide. The blue sequence in somatostatin represents a key pharmacophore in somatostatin, responsible for receptor binding. In somatostatin analogues, lysine (K) is conserved, while tryptophan is replaced with its stereoisomers in octreotide, lanreotide, vapreotide, and pasireotide. Phenylalanine is substituted with tyrosine, which has an additional hydroxyl group, and threonine is replaced with a more hydrophobic amino acid, such as valine, in lanreotide and vapreotide. Pasireotide incorporates the highest number of unnatural amino acids. In this analogue, cyclization occurs between the N- and C-terminal ends, while in octreotide, lanreotide, and vapreotide, cyclization involves the side chains of cysteine residues, similar to native somatostatin.
Figure Legend Snippet: On the top is the sequence of the native somatostatin peptide. The blue sequence in somatostatin represents a key pharmacophore in somatostatin, responsible for receptor binding. In somatostatin analogues, lysine (K) is conserved, while tryptophan is replaced with its stereoisomers in octreotide, lanreotide, vapreotide, and pasireotide. Phenylalanine is substituted with tyrosine, which has an additional hydroxyl group, and threonine is replaced with a more hydrophobic amino acid, such as valine, in lanreotide and vapreotide. Pasireotide incorporates the highest number of unnatural amino acids. In this analogue, cyclization occurs between the N- and C-terminal ends, while in octreotide, lanreotide, and vapreotide, cyclization involves the side chains of cysteine residues, similar to native somatostatin.

Techniques Used: Sequencing, Binding Assay, Analogues

Related Articles

Injection:

Article Title: Drug and Device News
Article Snippet: .. Source: Teva, August 30, 2017 Somatuline Depot For Carcinoid Syndrome Lanreotide injection 120 mg (Somatuline Depot, Ipsen Biopharmaceuticals, Inc.) has received FDA approval for the treatment of carcinoid syndrome. ..

other:

Article Title: Recent Progress in Drug Release Testing Methods of Biopolymeric Particulate System
Article Snippet: Somatuline Depot , Lanreotide acetate , Ipsen-Beafour , SC , Acromegaly (2007).

Article Title: Advances in Peptidomimetics for Next-Generation Therapeutics: Strategies, Modifications, and Applications
Article Snippet: lanreotide , Somatuline depot , somatostatin analogue (SSA) , 2007 , Ipsen , acromegaly, neuroendocrine tumors, and conditions with excess hormone secretion , SC.

Article Title: Impact of Formulation Parameters on In Vitro Release from Long-Acting Injectable Suspensions
Article Snippet: Degarelix acetate , Firmagon , SC , Ferring , Prostate cancer , 2008 , 80 mg base/vial; 120 mg base/vial: 28 days.

Binding Assay:

Article Title: Development and Challenges of Antimicrobial Peptides for Therapeutic Applications
Article Snippet: FIRMAGON , 12/24/2008 , 022201 , DEGARELIX ACETATE , FERRING , 1632.3 , Synthetic peptide , Prostate cancer treatment , Receptor binding , 53 h. .. SOMATULINE DEPOT , 30/08/2007 , 022074 , LANREOTIDE ACETATE , IPSEN PHARMA , 1096.34 , Cyclical octapeptide , Treatment of neuroendocrine tumors (NETs) and acromegaly , Receptor binding , 22 days. .. ERAXIS , 2/17/2006 , 021632 , ANIDULAFUNGIN , VICURON , 1140.3 , Lipopeptide , Anti-fungal drug , Inhibitor , 40–50 h.



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Ipsen Group somatuline depot
On the top is the sequence of the native somatostatin peptide. The blue sequence in somatostatin represents a key pharmacophore in somatostatin, responsible for receptor binding. In somatostatin analogues, lysine (K) is conserved, while tryptophan is replaced with its stereoisomers in octreotide, <t>lanreotide,</t> vapreotide, and pasireotide. Phenylalanine is substituted with tyrosine, which has an additional hydroxyl group, and threonine is replaced with a more hydrophobic amino acid, such as valine, in lanreotide and vapreotide. Pasireotide incorporates the highest number of unnatural amino acids. In this analogue, cyclization occurs between the N- and C-terminal ends, while in octreotide, lanreotide, and vapreotide, cyclization involves the side chains of cysteine residues, similar to native somatostatin.
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Preference for LAN administration setting . Survey population ( N = 80 with five missing values). Whiskers represent 95% confidence intervals. LAN, <t>lanreotide</t> autogel
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Preference for LAN administration setting . Survey population ( N = 80 with five missing values). Whiskers represent 95% confidence intervals. LAN, <t>lanreotide</t> autogel
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Patient disposition. a All participants from the screened population who met the inclusion/exclusion criteria and started to complete the survey. b All enrolled participants who completed the survey with no data quality concerns and irrespective of whether they had NETs or acromegaly; c 132 patients (97.1%) had received the branded formulation, and 4 patients (2.9%) had received the generic formulation. d Participants with at least 6 months’ experience of their current SSA treatment; e 122 participants (96.8%) had received the branded formulation, and 4 participants had received (3.2%) the generic formulation. f Participants who had been treated with both LAN and OCT. g All participants received the branded formulation. h Excluded participants from the USA as independent injection of <t>lanreotide</t> autogel is not approved in the USA. LAN lanreotide autogel/depot, NET neuroendocrine tumor, OCT octreotide long-acting release
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Image Search Results


On the top is the sequence of the native somatostatin peptide. The blue sequence in somatostatin represents a key pharmacophore in somatostatin, responsible for receptor binding. In somatostatin analogues, lysine (K) is conserved, while tryptophan is replaced with its stereoisomers in octreotide, lanreotide, vapreotide, and pasireotide. Phenylalanine is substituted with tyrosine, which has an additional hydroxyl group, and threonine is replaced with a more hydrophobic amino acid, such as valine, in lanreotide and vapreotide. Pasireotide incorporates the highest number of unnatural amino acids. In this analogue, cyclization occurs between the N- and C-terminal ends, while in octreotide, lanreotide, and vapreotide, cyclization involves the side chains of cysteine residues, similar to native somatostatin.

Journal: Chemical Reviews

Article Title: Advances in Peptidomimetics for Next-Generation Therapeutics: Strategies, Modifications, and Applications

doi: 10.1021/acs.chemrev.4c00989

Figure Lengend Snippet: On the top is the sequence of the native somatostatin peptide. The blue sequence in somatostatin represents a key pharmacophore in somatostatin, responsible for receptor binding. In somatostatin analogues, lysine (K) is conserved, while tryptophan is replaced with its stereoisomers in octreotide, lanreotide, vapreotide, and pasireotide. Phenylalanine is substituted with tyrosine, which has an additional hydroxyl group, and threonine is replaced with a more hydrophobic amino acid, such as valine, in lanreotide and vapreotide. Pasireotide incorporates the highest number of unnatural amino acids. In this analogue, cyclization occurs between the N- and C-terminal ends, while in octreotide, lanreotide, and vapreotide, cyclization involves the side chains of cysteine residues, similar to native somatostatin.

Article Snippet: lanreotide , Somatuline depot , somatostatin analogue (SSA) , 2007 , Ipsen , acromegaly, neuroendocrine tumors, and conditions with excess hormone secretion , SC.

Techniques: Sequencing, Binding Assay, Analogues

Pharmacokinetic profile (mean drug concentrations + SD) after a single application of prolonged-release lanreotide 90 mg (Somatuline Autogel ® ) in healthy volunteers (n = 13). The X-axis and Y-axis are segmented to show the profile of the product in the initial phase (Days 0–28). pAUC 0–7days , pAUC 7–28days , and pAUC 28-t are highlighted. Insert represents the full profile without axis scaling (adapted from ).

Journal: Pharmaceutics

Article Title: Partial AUCs in Long-Acting Injectables: Rationale, Challenges, Variability, Usefulness, and Clinical Relevance

doi: 10.3390/pharmaceutics17010021

Figure Lengend Snippet: Pharmacokinetic profile (mean drug concentrations + SD) after a single application of prolonged-release lanreotide 90 mg (Somatuline Autogel ® ) in healthy volunteers (n = 13). The X-axis and Y-axis are segmented to show the profile of the product in the initial phase (Days 0–28). pAUC 0–7days , pAUC 7–28days , and pAUC 28-t are highlighted. Insert represents the full profile without axis scaling (adapted from ).

Article Snippet: Lanreotide is a somatostatin analog formulated as an LAI product, administered via deep SC injection every 28 days (Somatuline ® depot, Ipsen Pharma SAS, and Somatuline ® Autogel, Ipsen Ltd., London, UK), used for the treatment of acromegaly and gastroenteropancreatic neuroendocrine tumors [ ].

Techniques:

Mean pAUCs (±SD) and intersubject variability (%) after a single application of prolonged-release lanreotide 90mg  (Somatuline  Autogel ® ) (n = 10). Data from [ <xref ref-type= 47 ]." width="100%" height="100%">

Journal: Pharmaceutics

Article Title: Partial AUCs in Long-Acting Injectables: Rationale, Challenges, Variability, Usefulness, and Clinical Relevance

doi: 10.3390/pharmaceutics17010021

Figure Lengend Snippet: Mean pAUCs (±SD) and intersubject variability (%) after a single application of prolonged-release lanreotide 90mg (Somatuline Autogel ® ) (n = 10). Data from [ 47 ].

Article Snippet: Lanreotide is a somatostatin analog formulated as an LAI product, administered via deep SC injection every 28 days (Somatuline ® depot, Ipsen Pharma SAS, and Somatuline ® Autogel, Ipsen Ltd., London, UK), used for the treatment of acromegaly and gastroenteropancreatic neuroendocrine tumors [ ].

Techniques:

List of marketed microsphere-based long-acting injectables

Journal: Drug Delivery and Translational Research

Article Title: Long-acting parenteral formulations of hydrophilic drugs, proteins, and peptide therapeutics: mechanisms, challenges, and therapeutic benefits with a focus on technologies

doi: 10.1007/s13346-024-01747-y

Figure Lengend Snippet: List of marketed microsphere-based long-acting injectables

Article Snippet: Somatuline Depot 60 mg , Ipsen , Lanreotide acetate , Acromegaly , 4 weeks , Spray drying , PLGA.

Techniques: Encapsulation, Polymer, Emulsion, Solvent, Evaporation

Preference for LAN administration setting . Survey population ( N = 80 with five missing values). Whiskers represent 95% confidence intervals. LAN, lanreotide autogel

Journal: Supportive Care in Cancer

Article Title: PREF-NET: a patient preference and experience study of lanreotide autogel administered in the home versus hospital setting among patients with gastroenteropancreatic neuroendocrine tumours in the UK

doi: 10.1007/s00520-024-08377-7

Figure Lengend Snippet: Preference for LAN administration setting . Survey population ( N = 80 with five missing values). Whiskers represent 95% confidence intervals. LAN, lanreotide autogel

Article Snippet: Somatuline® (lanreotide) Autogel®/Depot (Ipsen) (herein referred to as LAN) is a long-acting somatostatin analogue indicated for the treatment of functional symptoms associated with NETs.

Techniques:

Impact on activities of daily living with LAN administration at home versus hospital: integrated results from survey and interview populations . LAN, lanreotide autogel

Journal: Supportive Care in Cancer

Article Title: PREF-NET: a patient preference and experience study of lanreotide autogel administered in the home versus hospital setting among patients with gastroenteropancreatic neuroendocrine tumours in the UK

doi: 10.1007/s00520-024-08377-7

Figure Lengend Snippet: Impact on activities of daily living with LAN administration at home versus hospital: integrated results from survey and interview populations . LAN, lanreotide autogel

Article Snippet: Somatuline® (lanreotide) Autogel®/Depot (Ipsen) (herein referred to as LAN) is a long-acting somatostatin analogue indicated for the treatment of functional symptoms associated with NETs.

Techniques:

Patient disposition. a All participants from the screened population who met the inclusion/exclusion criteria and started to complete the survey. b All enrolled participants who completed the survey with no data quality concerns and irrespective of whether they had NETs or acromegaly; c 132 patients (97.1%) had received the branded formulation, and 4 patients (2.9%) had received the generic formulation. d Participants with at least 6 months’ experience of their current SSA treatment; e 122 participants (96.8%) had received the branded formulation, and 4 participants had received (3.2%) the generic formulation. f Participants who had been treated with both LAN and OCT. g All participants received the branded formulation. h Excluded participants from the USA as independent injection of lanreotide autogel is not approved in the USA. LAN lanreotide autogel/depot, NET neuroendocrine tumor, OCT octreotide long-acting release

Journal: Advances in Therapy

Article Title: PRESTO 2: An International Survey to Evaluate Patients’ Injection Experiences with the Latest Devices/Formulations of Long-Acting Somatostatin Analog Therapies for Neuroendocrine Tumors or Acromegaly

doi: 10.1007/s12325-022-02360-6

Figure Lengend Snippet: Patient disposition. a All participants from the screened population who met the inclusion/exclusion criteria and started to complete the survey. b All enrolled participants who completed the survey with no data quality concerns and irrespective of whether they had NETs or acromegaly; c 132 patients (97.1%) had received the branded formulation, and 4 patients (2.9%) had received the generic formulation. d Participants with at least 6 months’ experience of their current SSA treatment; e 122 participants (96.8%) had received the branded formulation, and 4 participants had received (3.2%) the generic formulation. f Participants who had been treated with both LAN and OCT. g All participants received the branded formulation. h Excluded participants from the USA as independent injection of lanreotide autogel is not approved in the USA. LAN lanreotide autogel/depot, NET neuroendocrine tumor, OCT octreotide long-acting release

Article Snippet: There are currently two proprietary (branded) injectable LA SSAs available for first-line treatment of NETs and acromegaly: Somatuline® (lanreotide) Autogel/Depot (Ipsen)—herein referred to as LAN—and Sandostatin® (octreotide) Long-Acting Release (Novartis)—herein referred to as OCT. LAN is provided as a ready-to-use prefilled syringe for administration by deep subcutaneous injection once every 28 days [ , ].

Techniques: Formulation, Injection

Proportion of patients with pain at injection site lasting > 2 days after most recent injection (Survey population a ). a All participants who completed the survey with no data quality concerns and irrespective of whether they had NETs or acromegaly. CI confidence interval, LAN lanreotide autogel/depot, NET neuroendocrine tumor, OCT octreotide long-acting release

Journal: Advances in Therapy

Article Title: PRESTO 2: An International Survey to Evaluate Patients’ Injection Experiences with the Latest Devices/Formulations of Long-Acting Somatostatin Analog Therapies for Neuroendocrine Tumors or Acromegaly

doi: 10.1007/s12325-022-02360-6

Figure Lengend Snippet: Proportion of patients with pain at injection site lasting > 2 days after most recent injection (Survey population a ). a All participants who completed the survey with no data quality concerns and irrespective of whether they had NETs or acromegaly. CI confidence interval, LAN lanreotide autogel/depot, NET neuroendocrine tumor, OCT octreotide long-acting release

Article Snippet: There are currently two proprietary (branded) injectable LA SSAs available for first-line treatment of NETs and acromegaly: Somatuline® (lanreotide) Autogel/Depot (Ipsen)—herein referred to as LAN—and Sandostatin® (octreotide) Long-Acting Release (Novartis)—herein referred to as OCT. LAN is provided as a ready-to-use prefilled syringe for administration by deep subcutaneous injection once every 28 days [ , ].

Techniques: Injection

Injection-site pain ( a ), injection-related issues ( b ) and technical injection problems ( c , d ) associated with LA SSA injection (Overall experience population a ). a Participants with at least 6 months’ experience with their current SSA treatment. b Participants were asked which symptoms/problems they had experienced—data are for those who experienced at least one issue (note that participants could choose more than one issue). c In participants who experienced technical problems (36 participants in the LAN group and 72 in the OCT group). CI confidence interval, LA long-acting, LAN lanreotide autogel/depot, OCT octreotide long-acting release, SSA somatostatin analog

Journal: Advances in Therapy

Article Title: PRESTO 2: An International Survey to Evaluate Patients’ Injection Experiences with the Latest Devices/Formulations of Long-Acting Somatostatin Analog Therapies for Neuroendocrine Tumors or Acromegaly

doi: 10.1007/s12325-022-02360-6

Figure Lengend Snippet: Injection-site pain ( a ), injection-related issues ( b ) and technical injection problems ( c , d ) associated with LA SSA injection (Overall experience population a ). a Participants with at least 6 months’ experience with their current SSA treatment. b Participants were asked which symptoms/problems they had experienced—data are for those who experienced at least one issue (note that participants could choose more than one issue). c In participants who experienced technical problems (36 participants in the LAN group and 72 in the OCT group). CI confidence interval, LA long-acting, LAN lanreotide autogel/depot, OCT octreotide long-acting release, SSA somatostatin analog

Article Snippet: There are currently two proprietary (branded) injectable LA SSAs available for first-line treatment of NETs and acromegaly: Somatuline® (lanreotide) Autogel/Depot (Ipsen)—herein referred to as LAN—and Sandostatin® (octreotide) Long-Acting Release (Novartis)—herein referred to as OCT. LAN is provided as a ready-to-use prefilled syringe for administration by deep subcutaneous injection once every 28 days [ , ].

Techniques: Injection

Journal: Advances in Therapy

Article Title: PRESTO 2: An International Survey to Evaluate Patients’ Injection Experiences with the Latest Devices/Formulations of Long-Acting Somatostatin Analog Therapies for Neuroendocrine Tumors or Acromegaly

doi: 10.1007/s12325-022-02360-6

Figure Lengend Snippet:

Article Snippet: There are currently two proprietary (branded) injectable LA SSAs available for first-line treatment of NETs and acromegaly: Somatuline® (lanreotide) Autogel/Depot (Ipsen)—herein referred to as LAN—and Sandostatin® (octreotide) Long-Acting Release (Novartis)—herein referred to as OCT. LAN is provided as a ready-to-use prefilled syringe for administration by deep subcutaneous injection once every 28 days [ , ].

Techniques: Analogues, Injection