Trial reportDrug design, development and therapy2012
A first-in-man study to evaluate the safety, tolerability, and pharmacokinetics of pasireotide (SOM230), a multireceptor-targeted somatostatin analog, in healthy volunteers.
Trial report in Drug design, development and therapy, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
19 citing papers in PubMed, 44 citations in OpenAlex.
- Paltusotine, a novel oral once-daily nonpeptide SST2 receptor agonist, suppresses GH and IGF-1 in healthy volunteers.Pituitary · 2022Trial
- Trial
- Quantification of the endogenous growth hormone and prolactin lowering effects of a somatostatin-dopamine chimera using population PK/PD modeling.Journal of pharmacokinetics and pharmacodynamics · 2020Trial
- Population Pharmacokinetics of Subcutaneous Pasireotide in Healthy Volunteers and Cushing's Disease Patients.Clinical pharmacokinetics · 2018Trial
- Effects of Subcutaneous Pasireotide on Cardiac Repolarization in Healthy Volunteers: a Single‐Center, Phase I, Randomized, Four‐Way Crossover Study.Journal of clinical pharmacology · 2014Trial
- Management of Diabetes Mellitus in Acromegaly and Cushing's Disease with Focus on Pasireotide Therapy: A Narrative Review.Diabetes, metabolic syndrome and obesity : targets and therapy · 2024Review
- The Effect of 6 Months' Treatment With Pasireotide LAR on Glucose Metabolism in Patients With Resistant Acromegaly in Real-World Clinical Settings.Frontiers in endocrinology · 2021Article
- A Low Dose of Pasireotide Prevents Hypoglycemia in Roux-en-Y Gastric Bypass-Operated Individuals.Obesity surgery · 2020Article
- Medical Treatment of Cushing's Disease: An Overview of the Current and Recent Clinical Trials.Frontiers in endocrinology · 2020Review
- Outcomes after Pancreatectomy with Routine Pasireotide Use.Journal of the American College of Surgeons · 2019Article
- Hyperglycemia induced by pasireotide in patients with Cushing's disease or acromegaly.Pituitary · 2016Review
- Article
- Successful Medical Treatment of Adult Nesidioblastosis With Pasireotide over 3 Years: A Case Report.Medicine · 2016Article
- Pasireotide in Acromegaly: A Review.Drugs · 2015Review
- Clinical use of pasireotide for Cushing's disease in adults.Therapeutics and clinical risk management · 2015Review
- Time and dose relationships between schisandrin B- and schisandrae fructus oil-induced hepatotoxicity and the associated elevations in hepatic and serum triglyceride levels in mice.Drug design, development and therapy · 2014Article
- Review
- Role of SST, CORT and ghrelin and its receptors at the endocrine pancreas.Frontiers in endocrinology · 2012Article
- Pasireotide for the Medical Management of Feline Hypersomatotropism.Journal of veterinary internal medicineArticle
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 3 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Pasireotide (SOM230) is a multireceptor-targeted somatostatin analog with high binding affinity for four of the five somatostatin receptor subtypes (sst(1,2,3) and sst(5)), and potential clinical activity in several neuroendocrine and oncologic conditions, including acromegaly, Cushing's disease, and neuroendocrine tumors (NET). This manuscript reports the first-in-man dose-escalation study of pasireotide, evaluating its safety, tolerability, and pharmacokinetics (PK) in healthy male volunteers. 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. PK and safety evaluations were carried out over 7 days post-dose. 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. Seventy-two subjects completed the study. Pasireotide was well tolerated with no serious adverse events observed at any dose. 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. The maximum tolerable dose was not established within the tested range. 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. GH suppression of 79%-96% was observed at single pasireotide doses between 200 μg and 1200 μg. In conclusion, pasireotide demonstrated favorable safety, tolerability, and PK profiles, as well as promising activity in suppressing the release of GH. The efficacy and safety of pasireotide is currently being evaluated in patients with acromegaly, Cushing's disease, NET, and various non-neuroendocrine disorders.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.