Trial reportPituitary2022
Paltusotine, a novel oral once-daily nonpeptide SST2 receptor agonist, suppresses GH and IGF-1 in healthy volunteers.
Trial report in Pituitary, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT03276858 (A Double-Blind, Randomized, Placebo-Controlled, Single- And-Multiple-Dose Study to Evaluate the Safety, PK, and PD of CRN00808 in Healthy Volunteers and to Determine the Effect of CRN00808 on Midazolam PK), which is not on this map. Cited by 21 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.
A Double-Blind, Randomized, Placebo-Controlled, Single- And-Multiple-Dose Study to Evaluate the Safety, PK, and PD of CRN00808 in Healthy Volunteers and to Determine the Effect of CRN00808 on Midazolam PK
Who cites it
21 citing papers in PubMed, 34 citations in OpenAlex.
- Trial
- Rapid and Sustained Response of Biochemically Uncontrolled Acromegaly to Once-daily Oral Paltusotine Treatment.The Journal of clinical endocrinology and metabolism · 2026Trial
- Acromegaly Disease Control Maintained After Switching From Injected Somatostatin Receptor Ligands to Oral Paltusotine.The Journal of clinical endocrinology and metabolism · 2024Trial
- ACROBAT Edge: Safety and Efficacy of Switching Injected SRLs to Oral Paltusotine in Patients With Acromegaly.The Journal of clinical endocrinology and metabolism · 2023Trial
- Phase 1 Study of Paltusotine, a Novel Oral Once‑Daily, Nonpeptide Selective Somatostatin Receptor 2 Agonist, in Healthy Japanese Adults.Clinical pharmacology in drug development · 2026Article
- Current treatment landscape of acromegaly.The Journal of clinical endocrinology and metabolism · 2026Review
- Paltusotine: The first FDA approved oral treatment for acromegaly.Annals of medicine and surgery (2012) · 2026Article
- The role of growth hormone in metastasis and angiogenesis of breast cancer.Bioscience reports · 2026Review
- Paltusotine: First Approval.Drugs · 2026Review
- A new era in oral treatment for acromegaly with the FDA-approved drug paltusotine.Annals of medicine and surgery (2012) · 2026Article
- Real-world burden of disease, treatment, and healthcare resource utilization in acromegaly: a quantitative survey of patient experiences.Journal of patient-reported outcomes · 2025Article
- An Update on Novel Pharmacotherapies for the Treatment of Neuroendocrine Tumors.International journal of molecular sciences · 2025Review
- Oral paltusotine, a nonpeptide selective somatostatin receptor 2 agonist: Mass balance, absolute bioavailability and metabolism in healthy participants.British journal of clinical pharmacology · 2025Article
- Paltusotine versus octreotide: different effects on radioligand uptake in neuroendocrine tumours.Endocrine oncology (Bristol, England) · 2025Article
- Exploring key features of selectivity in somatostatin receptors through molecular dynamics simulations.Computational and structural biotechnology journal · 2024Article
- Advances in the Oral Administration of Somatostatin Receptor Ligands in Acromegaly: A Systematic Review Focusing on Biochemical Response.Pharmaceutics · 2024Review
- Oral Octreotide Capsules and Paltusotine in Management of Acromegaly.TouchREVIEWS in endocrinology · 2024Review
- New Treatments for Acromegaly in Development.The Journal of clinical endocrinology and metabolism · 2024Article
- Prospect of acromegaly therapy: molecular mechanism of clinical drugs octreotide and paltusotine.Nature communications · 2023Article
- Discovery of Paltusotine (CRN00808), a Potent, Selective, and Orally Bioavailable Non-peptide SST2 Agonist.ACS medicinal chemistry letters · 2023Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
purposeEvaluate the pharmacodynamics, pharmacokinetics, and safety of paltusotine, an orally bioavailable, nonpeptide, somatostatin receptor subtype 2 (SST2) agonist being developed for the treatment of acromegaly and neuroendocrine tumors.
methodsA randomized, double-blind, placebo-controlled, single center, single and multiple ascending dose phase 1 study was conducted in healthy male volunteers who received (i) single-dose of oral paltusotine 1.25, 2.5, 5, 10, and 20 mg (solution); and 40 and 60 mg (capsules) or (ii) multiple-dose oral paltusotine capsules once daily 5 mg (× 7 days), 10, 20, and 30 mg (× 10 days). Main outcome measures were pharmacodynamics (changes in growth hormone-releasing hormone [GHRH] stimulated growth hormone [GH] and insulin-like growth factor 1 [IGF-1]), pharmacokinetics, safety, and tolerability.
resultsSingle-dose cohorts: n = 41 active, n = 14 placebo. Multiple-dose cohorts: n = 24 active, n = 12 placebo. Paltusotine was well tolerated, orally bioavailable, associated with increased plasma concentrations to doses up to 40 mg, and was eliminated with a half-life of approximately 30 h. Single-dose paltusotine 1.25 to 20 mg suppressed GHRH-stimulated GH secretion by 44% to 93% compared to 15% with placebo. Multiple-dose paltusotine 5 to 30 mg administered once daily for 10 days suppressed IGF-1 by 19% to 37% compared to an increase of 2.4% with placebo.
conclusionsPaltusotine suppresses GH and IGF-1 in a dose-dependent fashion, with a safety profile similar to currently approved SST2 receptor ligands. Paltusotine is a promising once-daily oral nonpeptide SST2 agonist candidate for managing acromegaly and neuroendocrine tumors.
trial registrationNCT03276858, registered September 8, 2017, retrospectively registered.
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What OpenQuestion holds
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.