Safety, tolerability, pharmacokinetics, and pharmacodynamics of a long-acting release (LAR) formulation of pasireotide (SOM230) in patients with gastroenteropancreatic neuroendocrine tumors: results from a randomized, multicenter, open-label, phase I study.

Wolin EM, Hu K, Hughes G, Bouillaud E, Giannone V, Resendiz KH

Cancer chemotherapy and pharmacology14 Jun 2013Cited by 30 (Europe PMC)

PMID23765178PMCIDPMC3719006DOI10.1007/s00280-013-2202-1PepBankPUB-23765178

Summary

PurposePasireotide (SOM230), a novel multireceptor ligand somatostatin analog (SSA), binds with high affinity to four of the five somatostatin receptor subtypes (sst1-3, 5). This study evaluated the safety, tolerability, pharmacokinetics, and pharmacodynamics profiles of pasireotide long-acting release (LAR) formulation in patients with advanced gastroenteropancreatic neuroendocrine tumor (GEP NET) refractory to other SSAs.MethodsIn this randomized, multicenter, open-label, phase II study, patients with biopsy-proven primary or metastatic GEP NET refractory to available SSAs were randomly assigned 1:1:1 to receive pasireotide LAR by deep intragluteal injection at a dose of 20, 40, or 60 mg once every 28 days for 3 months.ResultsForty-two patients received pasireotide LAR. Adverse events were reported by 34 (81 %) patients, with the most frequently reported including diarrhea, fatigue, abdominal pain, and nausea. Mean fasting glucose levels were increased compared with baseline at all points throughout the study. After the third injection of pasireotide LAR, the median trough plasma concentrations on day 84 were 4.82, 12.0, and 19.7 ng/mL in the 20-, 40-, and 60-mg treatment groups, respectively. Drug accumulation was limited for each dose based on the increase in trough concentrations after the first to third injections (accumulation ratios were approximately 1 from all dose levels).ConclusionsThis study demonstrated that a new, once-monthly, intramuscular LAR formulation of pasireotide was well tolerated in patients with advanced GEP NET. Steady state levels of plasma pasireotide were achieved after three injections.

CC BYText from Europe PMC. Highlighted sentences are the source of results.

Results from this study10

10 results from studies that gave the peptide. 10 results from people.

01HumanNon-randomized trialSafety outcome
In patients with advanced GEP NET, 34 (81 %) reported adverse events during pasireotide LAR treatment.
In plain wordsIn patients with advanced GEP NET, 81 % reported side effects during pasireotide LAR treatment.
Peptide
Pasireotide
Outcome
Not applicableAny adverse event
Study
n = 42
Outcome group
Adverse events · Whole body
Studied dose
20, 40, or 60 mg once every 28 days · deep intragluteal injection · 3 monthsAs given in this study (human).
Measurements
Patients with any adverse event
34 patients
pasireotide LAR, GEP NET patients
Proportion with any adverse event
81%
pasireotide LAR, GEP NET patients
Source sentences
Summary
Adverse events were reported by 34 (81 %) patients, with the most frequently reported including diarrhea, fatigue, abdominal pain, and nausea.
2 context sentences(design, population, supporting numbers)
Summary · context
Forty-two patients received pasireotide LAR.
Summary · context
In this randomized, multicenter, open-label, phase II study, patients with biopsy-proven primary or metastatic GEP NET refractory to available SSAs were randomly assigned 1:1:1 to receive pasireotide LAR by deep intragluteal injection at a dose of 20, 40, or 60 mg once every 28 days for 3 months.
Show in the study text Report a problemFND-2376517801
02HumanNon-randomized trialSafety outcome
In patients with advanced GEP NET, diarrhea was among the most frequent adverse events with pasireotide LAR.
In plain wordsPatients with advanced GEP NET frequently reported diarrhea during pasireotide LAR treatment.
Peptide
Pasireotide
Outcome
Not applicableDiarrhea
Study
n = 42
Outcome group
Gastrointestinal adverse events · Gastrointestinal
Studied dose
20, 40, or 60 mg once every 28 days · deep intragluteal injection · 3 monthsAs given in this study (human).
Source sentences
Summary
Adverse events were reported by 34 (81 %) patients, with the most frequently reported including diarrhea, fatigue, abdominal pain, and nausea.
1 context sentence(design, population, supporting numbers)
Summary · context
In this randomized, multicenter, open-label, phase II study, patients with biopsy-proven primary or metastatic GEP NET refractory to available SSAs were randomly assigned 1:1:1 to receive pasireotide LAR by deep intragluteal injection at a dose of 20, 40, or 60 mg once every 28 days for 3 months.
Show in the study text Report a problemFND-2376517802
03HumanNon-randomized trialSafety outcome
In patients with advanced GEP NET, fatigue was among the most frequent adverse events with pasireotide LAR.
In plain wordsPatients with advanced GEP NET frequently reported fatigue during pasireotide LAR treatment.
Peptide
Pasireotide
Outcome
Not applicableFatigue
Study
n = 42
Outcome group
Adverse events · Whole body
Studied dose
20, 40, or 60 mg once every 28 days · deep intragluteal injection · 3 monthsAs given in this study (human).
Source sentences
Summary
Adverse events were reported by 34 (81 %) patients, with the most frequently reported including diarrhea, fatigue, abdominal pain, and nausea.
1 context sentence(design, population, supporting numbers)
Summary · context
In this randomized, multicenter, open-label, phase II study, patients with biopsy-proven primary or metastatic GEP NET refractory to available SSAs were randomly assigned 1:1:1 to receive pasireotide LAR by deep intragluteal injection at a dose of 20, 40, or 60 mg once every 28 days for 3 months.
Show in the study text Report a problemFND-2376517803
04HumanNon-randomized trialSafety outcome
In patients with advanced GEP NET, abdominal pain was among the most frequent adverse events with pasireotide LAR.
In plain wordsPatients with advanced GEP NET frequently reported abdominal pain during pasireotide LAR treatment.
Peptide
Pasireotide
Outcome
Not applicableAbdominal pain
Study
n = 42
Outcome group
Gastrointestinal adverse events · Gastrointestinal
Studied dose
20, 40, or 60 mg once every 28 days · deep intragluteal injection · 3 monthsAs given in this study (human).
Source sentences
Summary
Adverse events were reported by 34 (81 %) patients, with the most frequently reported including diarrhea, fatigue, abdominal pain, and nausea.
1 context sentence(design, population, supporting numbers)
Summary · context
In this randomized, multicenter, open-label, phase II study, patients with biopsy-proven primary or metastatic GEP NET refractory to available SSAs were randomly assigned 1:1:1 to receive pasireotide LAR by deep intragluteal injection at a dose of 20, 40, or 60 mg once every 28 days for 3 months.
Show in the study text Report a problemFND-2376517804
05HumanNon-randomized trialSafety outcome
In patients with advanced GEP NET, nausea was among the most frequent adverse events with pasireotide LAR.
In plain wordsPatients with advanced GEP NET frequently reported nausea during pasireotide LAR treatment.
Peptide
Pasireotide
Outcome
Not applicableNausea
Study
n = 42
Outcome group
Gastrointestinal adverse events · Gastrointestinal
Studied dose
20, 40, or 60 mg once every 28 days · deep intragluteal injection · 3 monthsAs given in this study (human).
Source sentences
Summary
Adverse events were reported by 34 (81 %) patients, with the most frequently reported including diarrhea, fatigue, abdominal pain, and nausea.
1 context sentence(design, population, supporting numbers)
Summary · context
In this randomized, multicenter, open-label, phase II study, patients with biopsy-proven primary or metastatic GEP NET refractory to available SSAs were randomly assigned 1:1:1 to receive pasireotide LAR by deep intragluteal injection at a dose of 20, 40, or 60 mg once every 28 days for 3 months.
Show in the study text Report a problemFND-2376517805
06HumanNon-randomized trialSafety outcome
In patients with advanced GEP NET, mean fasting glucose increased from baseline at all study points during pasireotide LAR treatment.
In plain wordsIn patients with advanced GEP NET, fasting blood sugar increased from baseline during pasireotide LAR treatment.
Peptide
Pasireotide
Outcome
IncreaseFasting glucose
Study
n: not reported in source
Outcome group
Glycemic control · Metabolic and weight
Studied dose
20, 40, or 60 mg once every 28 days · deep intragluteal injection · 3 monthsAs given in this study (human).
Source sentences
Summary
Mean fasting glucose levels were increased compared with baseline at all points throughout the study.
1 context sentence(design, population, supporting numbers)
Summary · context
In this randomized, multicenter, open-label, phase II study, patients with biopsy-proven primary or metastatic GEP NET refractory to available SSAs were randomly assigned 1:1:1 to receive pasireotide LAR by deep intragluteal injection at a dose of 20, 40, or 60 mg once every 28 days for 3 months.
Show in the study text Report a problemFND-2376517806
07HumanNon-randomized trialPharmacokinetics
In patients with advanced GEP NET, median pasireotide LAR trough concentration was 4.82 ng/mL on day 84 with 20 mg.
In plain wordsIn patients with advanced GEP NET, the 20-mg pasireotide LAR group had a median trough concentration of 4.82 ng/mL.
Peptide
Pasireotide
Outcome
Not applicableDay 84 trough concentration, 20 mg
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
20 mg once every 28 days · deep intragluteal injection · 3 monthsAs given in this study (human).
Measurements
Median trough plasma concentration, day 84
4.82 ng/mL
pasireotide LAR 20 mg every 28 days, after third injection
Source sentences
Summary
After the third injection of pasireotide LAR, the median trough plasma concentrations on day 84 were 4.82, 12.0, and 19.7 ng/mL in the 20-, 40-, and 60-mg treatment groups, respectively.
1 context sentence(design, population, supporting numbers)
Summary · context
In this randomized, multicenter, open-label, phase II study, patients with biopsy-proven primary or metastatic GEP NET refractory to available SSAs were randomly assigned 1:1:1 to receive pasireotide LAR by deep intragluteal injection at a dose of 20, 40, or 60 mg once every 28 days for 3 months.
Show in the study text Report a problemFND-2376517807
08HumanNon-randomized trialPharmacokinetics
In patients with advanced GEP NET, median pasireotide LAR trough concentration was 12.0 ng/mL on day 84 with 40 mg.
In plain wordsIn patients with advanced GEP NET, the 40-mg pasireotide LAR group had a median trough concentration of 12.0 ng/mL.
Peptide
Pasireotide
Outcome
Not applicableDay 84 trough concentration, 40 mg
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
40 mg once every 28 days · deep intragluteal injection · 3 monthsAs given in this study (human).
Measurements
Median trough plasma concentration, day 84
12 ng/mL
pasireotide LAR 40 mg every 28 days, after third injection
Source sentences
Summary
After the third injection of pasireotide LAR, the median trough plasma concentrations on day 84 were 4.82, 12.0, and 19.7 ng/mL in the 20-, 40-, and 60-mg treatment groups, respectively.
1 context sentence(design, population, supporting numbers)
Summary · context
In this randomized, multicenter, open-label, phase II study, patients with biopsy-proven primary or metastatic GEP NET refractory to available SSAs were randomly assigned 1:1:1 to receive pasireotide LAR by deep intragluteal injection at a dose of 20, 40, or 60 mg once every 28 days for 3 months.
Show in the study text Report a problemFND-2376517808
09HumanNon-randomized trialPharmacokinetics
In patients with advanced GEP NET, median pasireotide LAR trough concentration was 19.7 ng/mL on day 84 with 60 mg.
In plain wordsIn patients with advanced GEP NET, the 60-mg pasireotide LAR group had a median trough concentration of 19.7 ng/mL.
Peptide
Pasireotide
Outcome
Not applicableDay 84 trough concentration, 60 mg
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
60 mg once every 28 days · deep intragluteal injection · 3 monthsAs given in this study (human).
Measurements
Median trough plasma concentration, day 84
19.7 ng/mL
pasireotide LAR 60 mg every 28 days, after third injection
Source sentences
Summary
After the third injection of pasireotide LAR, the median trough plasma concentrations on day 84 were 4.82, 12.0, and 19.7 ng/mL in the 20-, 40-, and 60-mg treatment groups, respectively.
1 context sentence(design, population, supporting numbers)
Summary · context
In this randomized, multicenter, open-label, phase II study, patients with biopsy-proven primary or metastatic GEP NET refractory to available SSAs were randomly assigned 1:1:1 to receive pasireotide LAR by deep intragluteal injection at a dose of 20, 40, or 60 mg once every 28 days for 3 months.
Show in the study text Report a problemFND-2376517809
10HumanNon-randomized trialPharmacokinetics
In patients with advanced GEP NET, pasireotide LAR accumulation ratios were approximately 1 at all doses from the first to third injections.
In plain wordsIn patients with advanced GEP NET, pasireotide LAR showed limited accumulation between the first and third injections.
Peptide
Pasireotide
Outcome
Not applicableDrug accumulation
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
20, 40, or 60 mg once every 28 days · deep intragluteal injection · 3 monthsAs given in this study (human).
Measurements
Accumulation ratio
≈ 1 ratio
pasireotide LAR, all dose levels, first to third injection
Source sentences
Summary
Drug accumulation was limited for each dose based on the increase in trough concentrations after the first to third injections (accumulation ratios were approximately 1 from all dose levels).
1 context sentence(design, population, supporting numbers)
Summary · context
In this randomized, multicenter, open-label, phase II study, patients with biopsy-proven primary or metastatic GEP NET refractory to available SSAs were randomly assigned 1:1:1 to receive pasireotide LAR by deep intragluteal injection at a dose of 20, 40, or 60 mg once every 28 days for 3 months.
Show in the study text Report a problemFND-2376517810

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28 Oct 2026, 02:03 UTC
Study results updated
Version 1
27 Oct 2026, 16:34 UTC
First added · source update from Europe PMC

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