A first-in-man study to evaluate the safety, tolerability, and pharmacokinetics of pasireotide (SOM230), a multireceptor-targeted somatostatin analog, in healthy volunteers.

Golor G, Hu K, Ruffin M, Buchelt A, Bouillaud E, Wang Y, Maldonado M

Drug design, development and therapy19 Apr 2012Cited by 35 (Europe PMC)

PMID22573933PMCIDPMC3346155DOI10.2147/dddt.s29125PepBankPUB-22573933

Read at source PubMedAsk about this study

Summary

The text of this summary is not shown here, because the article license does not allow reuse. Read it at the source (opens in a new tab)

Text rights: CC BY-NC. Results still quote short attributed sentences.

Results from this study8

8 results from studies that gave the peptide. 8 results from people.

01HumanNon-randomized trialSafety outcome
In healthy men, no serious adverse events occurred at any pasireotide dose.
In plain wordsHealthy men had no serious side effects at any tested pasireotide dose.
Peptide
Pasireotide
Outcome
Not applicableSerious adverse events
Study
n: not reported in source
Outcome group
Adverse events · Whole body
Studied dose
1-1200 μg single dose · subcutaneousAs given in this study (human).
Source sentences
Summary
Pasireotide was well tolerated with no serious adverse events observed at any dose.
2 context sentences(design, population, supporting numbers)
Summary · context
A single dose of pasireotide 1-1200 μg was administered subcutaneously in four to eight subjects per dose level, with two additional subjects per cohort administered placebo.
Summary · context
PK and safety evaluations were carried out over 7 days post-dose.
Report a problemFND-2257393301
02HumanNon-randomized trialSafety outcome
In healthy men, transient blood glucose elevations were observed 2-6 hours after pasireotide 200-1200 μg and resolved without intervention by 23 hours post-dose.
In plain wordsIn healthy men, blood sugar rose temporarily after pasireotide 200-1200 μg and settled without intervention by 23 hours.
Peptide
Pasireotide
Outcome
IncreaseTransient blood glucose elevation
Study
n: not reported in source
Outcome group
Glycemic control · Metabolic and weight
Studied dose
200-1200 μg single dose · subcutaneousAs given in this study (human).
Source sentences
Summary
Transient elevations in blood glucose levels were observed 2-6 hours after administration of pasireotide at doses between 200 μg and 1200 μg, but this resolved without intervention by 23 hours post-dosing.
2 context sentences(design, population, supporting numbers)
Summary · context
A single dose of pasireotide 1-1200 μg was administered subcutaneously in four to eight subjects per dose level, with two additional subjects per cohort administered placebo.
Summary · context
PK and safety evaluations were carried out over 7 days post-dose.
Report a problemFND-2257393302
03HumanNon-randomized trialSafety outcome
In healthy men, the maximum tolerable pasireotide dose was not established within the tested range.
In plain wordsIn healthy men, the study did not establish the highest tolerable pasireotide dose.
Peptide
Pasireotide
Outcome
Direction not reportedMaximum tolerable dose
Study
n: not reported in source
Outcome group
Adverse events · Whole body
Studied dose
1-1200 μg single dose · subcutaneousAs given in this study (human).
Source sentences
Summary
The maximum tolerable dose was not established within the tested range.
2 context sentences(design, population, supporting numbers)
Summary · context
A single dose of pasireotide 1-1200 μg was administered subcutaneously in four to eight subjects per dose level, with two additional subjects per cohort administered placebo.
Summary · context
PK and safety evaluations were carried out over 7 days post-dose.
Report a problemFND-2257393303
04HumanNon-randomized trialPharmacokinetics
In healthy men, pasireotide t(max) was 0.25-0.5 hours.
In plain wordsIn healthy men, pasireotide reached peak levels in 0.25-0.5 hours.
Peptide
Pasireotide
Outcome
Not applicableAbsorption time
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
1-1200 μg single dose · subcutaneousAs given in this study (human).
Measurements
tmax
0.25 to 0.5 hours
single pasireotide doses 1-1200 μg, healthy male volunteers
Source sentences
Summary
Pasireotide demonstrated a favorable PK profile with fast absorption (t(max): 0.25-0.5 hours), low clearance (CL/F: 8-13 L/hour), long effective elimination half-life (mean t(½,β): 7-11 hours), and a proportional dose-exposure relationship.
2 context sentences(design, population, supporting numbers)
Summary · context
A single dose of pasireotide 1-1200 μg was administered subcutaneously in four to eight subjects per dose level, with two additional subjects per cohort administered placebo.
Summary · context
PK and safety evaluations were carried out over 7 days post-dose.
Report a problemFND-2257393304
05HumanNon-randomized trialPharmacokinetics
In healthy men, pasireotide CL/F was 8-13 L/hour.
In plain wordsIn healthy men, pasireotide clearance was 8-13 L/hour.
Peptide
Pasireotide
Outcome
Not applicableClearance
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
1-1200 μg single dose · subcutaneousAs given in this study (human).
Measurements
CL/F
8 to 13 L/hour
single pasireotide doses 1-1200 μg, healthy male volunteers
Source sentences
Summary
Pasireotide demonstrated a favorable PK profile with fast absorption (t(max): 0.25-0.5 hours), low clearance (CL/F: 8-13 L/hour), long effective elimination half-life (mean t(½,β): 7-11 hours), and a proportional dose-exposure relationship.
2 context sentences(design, population, supporting numbers)
Summary · context
A single dose of pasireotide 1-1200 μg was administered subcutaneously in four to eight subjects per dose level, with two additional subjects per cohort administered placebo.
Summary · context
PK and safety evaluations were carried out over 7 days post-dose.
Report a problemFND-2257393305
06HumanNon-randomized trialPharmacokinetics
In healthy men, pasireotide mean effective elimination half-life was 7-11 hours.
In plain wordsIn healthy men, pasireotide effective elimination half-life averaged 7-11 hours.
Peptide
Pasireotide
Outcome
Not applicableEffective elimination half-life
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
1-1200 μg single dose · subcutaneousAs given in this study (human).
Measurements
Mean effective elimination half-life t(½,β)
7 to 11 hours
single pasireotide doses 1-1200 μg, healthy male volunteers
Source sentences
Summary
Pasireotide demonstrated a favorable PK profile with fast absorption (t(max): 0.25-0.5 hours), low clearance (CL/F: 8-13 L/hour), long effective elimination half-life (mean t(½,β): 7-11 hours), and a proportional dose-exposure relationship.
2 context sentences(design, population, supporting numbers)
Summary · context
A single dose of pasireotide 1-1200 μg was administered subcutaneously in four to eight subjects per dose level, with two additional subjects per cohort administered placebo.
Summary · context
PK and safety evaluations were carried out over 7 days post-dose.
Report a problemFND-2257393306
07HumanNon-randomized trialPharmacokinetics
In healthy men, pasireotide showed a proportional dose-exposure relationship.
In plain wordsIn healthy men, pasireotide exposure increased in proportion to dose.
Peptide
Pasireotide
Outcome
IncreaseDose-exposure relationship
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
1-1200 μg single dose · subcutaneousAs given in this study (human).
Source sentences
Summary
Pasireotide demonstrated a favorable PK profile with fast absorption (t(max): 0.25-0.5 hours), low clearance (CL/F: 8-13 L/hour), long effective elimination half-life (mean t(½,β): 7-11 hours), and a proportional dose-exposure relationship.
2 context sentences(design, population, supporting numbers)
Summary · context
A single dose of pasireotide 1-1200 μg was administered subcutaneously in four to eight subjects per dose level, with two additional subjects per cohort administered placebo.
Summary · context
PK and safety evaluations were carried out over 7 days post-dose.
Report a problemFND-2257393307
08HumanNon-randomized trialActivity measurement
In healthy men, single pasireotide doses of 200-1200 μg suppressed growth hormone by 79%-96%.
In plain wordsIn healthy men, single pasireotide doses suppressed growth hormone by 79%-96%.
Peptide
Pasireotide
Outcome
DecreaseGrowth hormone suppression
Study
n: not reported in source
Outcome group
Growth hormone and IGF-1 · Endocrine and hormones
Studied dose
200-1200 μg single dose · subcutaneousAs given in this study (human).
Measurements
GH suppression
79 to 96%
single pasireotide doses 200-1200 μg, healthy male volunteers
Source sentences
Summary
GH suppression of 79%-96% was observed at single pasireotide doses between 200 μg and 1200 μg.
3 context sentences(design, population, supporting numbers)
Summary · context
Growth hormone (GH) suppression was evaluated using a GH-releasing hormone stimulation test on Day -1 and Day 1 at 3-5 hours post-injection.
Summary · context
A single dose of pasireotide 1-1200 μg was administered subcutaneously in four to eight subjects per dose level, with two additional subjects per cohort administered placebo.
Summary · context
PK and safety evaluations were carried out over 7 days post-dose.
Report a problemFND-2257393308

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

Version 2Current
28 Oct 2026, 02:03 UTC
Study results updated
Version 1
27 Oct 2026, 16:34 UTC
First added · source update from Europe PMC

Subjects

Terms as the source lists them.

Publication types

MeSH terms

Keywords

PepBank is a research reference. Talk to a doctor before you use any peptide.