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octreotide acetate (OOA / oral octreotide / Octreolin)

✓ Approved

Chiasma, Inc. · SSTR2 · 小分子

什么是 octreotide acetate？

octreotide acetate 是一种小分子，由Chiasma, Inc.研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名OOA, oral octreotide, Octreolin
公司Chiasma, Inc.
药物类别小分子, 多肽类
分子靶点SSTR2, SSTR5
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Chiasma, Inc.

作用机制

分子靶点

octreotide acetate 作用于 2 个分子靶点：

SSTR2somatostatin receptor 2 (SST2)
SSTR5somatostatin receptor 5 (SST5, SS-5-R)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

octreotide acetate 针对 6 个适应症，涉及 4 个治疗领域。

治疗领域疾病/病症分期
Endocrine disordersAcromegaly✓ Approved
Endocrine disordersCarcinoid syndromePhase II
Hepatobiliary disordersPortal hypertensionPhase II
Vascular disordersHypertensionPhase I
Gastrointestinal disordersPancreatitisPhase I

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相关研究文献

PubMedInternational journal of pharmaceutics2026-07-27

Impact of dosage form on the pharmacokinetics of octreotide after oral administration with permeation enhancers.

Fredholt Freja F, Raptis Konstantinos K, Rønholt Stine S, Hofmann Michael M et al.

The permeation enhancers (PEs) sodium salcaprozate (SNAC) and sodium decanoate (C10) are reported to enhance gastric and intestinal absorption of different macromolecules. While previous preclinical and clinical studies report effects of these PEs, no head-to-head comparison between their effect in different dosage forms administered by oral gavage in rats is reported. For that purpose, we developed mini-tablets containing octreotide and SNAC or C10 as the PE. The disintegration behavior of the mini-tablets was evaluated using biorelevant liquid volumes of 0.1-0.5 mL in different experimental setups. The efficacy of the PEs co-administered in solution and the in solid dosage form was compared in rats after oral gavage and subsequent assessment of the octreotide pharmacokinetics (PK). While the type of PE and the volume only slightly affected the disintegration time for the mini-tablets, significant differences were observed to depend on the exact experimental setup. Upon oral gavage, plasma octreotide concentrations were enhanced in presence of PE for both solution and mini-tablet formulations compared to control formulations without PEs, as reflected by the higher area under the plasma concentration curves (AUC). SNAC produced a significantly greater relative bioavailability than both the control and the C10-containing formulations. The relative bioavailability increased 2.0- and 9.4-fold for C10 and SNAC solutions, respectively. Notably, the mini-tablets both with and without PE showed higher numerical octreotide absorption than their solution counterparts and the mini-tablets resulted in a 1.6- and 1.8-fold increase for C10, and a 4.8- and 5.4-fold increase for SNAC in relative bioavailability after co-administering with low and high liquid volumes, respectively. In conclusion, the study shows that the PK profiles for octreotide are different after oral gavage administration of solutions compared to mini-tablets containing the PEs SNAC and C10 and that SNAC outperformed C10 as a permeation enhancer when administered by oral gavage.

PMID 42503373
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PubMedJournal of bacteriology2026-07-27

Oxygen-dependent partitioning of acetate assimilation via Acs and AckA-Pta pathways in Pseudomonas aeruginosa.

Watkins M E ME, Tonapi K V KV, VanDrisse C M CM

Pseudomonas aeruginosa is a metabolically versatile pathogen that thrives in host environments characterized by gradients of oxygen and nutrient availability. Although acetate is an abundant carbon source in chronic infections, the mechanisms governing P. aeruginosa acetate assimilation remains poorly understood. In many bacteria, acetate utilization occurs via the low-carbon-flux acetyl-CoA synthetase (Acs) or the high-carbon-flux acetate kinase/phosphotransacetylase (AckA-Pta) pathways. Here, we show that in P. aeruginosa, the above-mentioned pathways assimilate acetate as a function of oxygen availability, not as a function of carbon concentration. Our growth data demonstrate that AcsA is required for robust growth on acetate under oxic conditions, whereas the AckA-Pta pathway is essential for robust growth on acetate under anoxic conditions. Complementation experiments reveal that both pathways are functionally capable of acetate assimilation regardless of oxygen presence, indicating that pathway usage is primarily controlled by transcriptional regulation. Consistent with this, RT-qPCR analysis shows that acsA expression was elevated under oxic conditions, while ackA and pta were upregulated in the absence of oxygen. Despite these regulatory differences, kinetic analyses demonstrated that Acs and AckA from P. aeruginosa exhibit substrate affinities and catalytic efficiencies comparable to those of Salmonella enterica, indicating that the ability of both pathways to support P. aeruginosa growth across acetate concentrations is not due to altered enzyme kinetics like in other organisms. Together, these findings establish a new model in which oxygen availability, rather than acetate concentration, governs acetate assimilation in P. aeruginosa, with important implications for metabolic adaptation during infection. Recent work has highlighted metabolic regulation as a driver of virulence, yet how P. aeruginosa metabolizes key metabolites found at infection sites remains uncharacterized. P. aeruginosa has a strong preference for acetate over other conventional carbon sources such as glucose, and acetate is found at millimolar concentrations in hosts. However, how P. aeruginosa regulates pathways involved in acetate assimilation remains largely unknown. Because steep oxygen gradients exist in host niches, where P. aeruginosa encounters acetate, understanding how acetate assimilation pathways are regulated via oxygen tension is essential for identifying spatial vulnerabilities at infection sites.

PMID 42505140
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PubMedJournal of fungi (Basel, Switzerland)2026-07-27

Acetate Signalling Regulates Virulence-Associated Traits in the Esca Pathogen Phaeomoniella chlamydospora.

Novák Ádám Á, Szabó Dóra D, Gomba-Tóth Adrienn A, Molnár Nikolett N et al.

Phaeomoniella chlamydospora (Pch) is a pioneer pathogen of esca, one of the most destructive grapevine trunk diseases worldwide. A recent work suggests that acetate may act as a quorum-sensing (QS) molecule in Pch, promoting biofilm formation in a concentration-dependent manner. However, the broader influence of acetate on virulence-associated traits remains unexplored. In this study, three Pch isolates were cultured under increasing sodium acetate concentrations (0-100 mM) and assessed for pigmentation, extracellular enzyme activities (amylase, cellulase, protease, esterase, and pectinase), phenolic compound-degrading capacity, and antibacterial activity against a grapevine-associated Pseudomonas sp. isolate. Pigmentation, as well as amylase and cellulase activities, were significantly increased at low acetate supplement levels (6.25-12.5 mM), while esterase activity was unaffected. The expression of these traits decreased above 25 mM acetate supplementation. Phenolic compound degradation capacity, antibacterial efficacy, as well as protease and pectinase activities progressively suppressed at all acetate concentrations. These results indicate that acetate concentration modulates multiple virulence-associated phenotypes of Pch in vitro. Based on these patterns, we propose a hypothetical model in which acetate-dependent phenotypic changes may reflect a shift between establishment-associated activities and reduced extracellular activity at higher acetate levels. This model remains to be validated by mechanistic and in planta infection-based studies.

PMID 42506300
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PubMedInorganic chemistry2026-07-27

Functionalization of β-Alkylcorrole Using Ag(I) Salts.

Marsotto Martina M, Pomarico Giuseppe G, Stefanelli Manuela M, Troiani Anna A et al.

To date, the coordination chemistry of β-alkylcorroles is significantly less developed than that of their triaryl analogues. To address this gap, we investigated the seemingly straightforward synthesis of silver complexes of β-alkylcorroles, employing a procedure previously reported for Ag(III) insertion into meso-triarylcorroles. However, when AgOAc was used as the silver source in pyridine, the reaction resulted in the formation of oxidation products, specifically oxocorroles. In acetonitrile, a broader distribution of products was observed, yielding compounds in addition to oxocorroles. Characterization through UV-vis spectroscopy, 1H NMR, mass spectrometry, and single-crystal X-ray crystallography revealed the formation of an acetate-functionalized oxocorrole, along with a second species resulting from simultaneous silver insertion and acetate incorporation at the meso-position. Substituting AgOAc with AgNO2 demonstrated a marked time dependence: rapid and complete meso nitration occurred within minutes, while extended reaction times also facilitated silver insertion into the preformed trinitrocorrole free base. The use of silver salts with non-nucleophilic anions (e.g., AgPF6 and AgNO3) did not yield either metalation or meso-functionalization. These results suggest that the coordination of the silver ion into the corrole core is almost permitted only after peripheral substitution, highlighting the distinct reactivity of alkylcorroles compared to their triaryl counterparts.

PMID 42504884
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PubMedACS applied materials & interfaces2026-07-27

Electrospun Cellulose Acetate Membranes Enable Low-Background Fluorescent Nanodiamond Lateral Flow Immunoassays for Highly Sensitive cTnI Detection.

Ren Zixuan Z, Xu Weimin W, Zhao Jiajia J, Cui Yue Y

Lateral flow immunoassays (LFAs) are widely used because of their simplicity, rapid readout, and low cost; however, quantitative performance is often limited by insufficient signal intensity and background interference from the membrane substrate. This issue becomes more severe when high-brightness fluorescent nanolabels are introduced: conventional nitrocellulose (NC) membranes tend to exhibit autofluorescence and strong light scattering and can also promote nonspecific retention of nanoparticles, which elevates background and compromises quantitative reliability. Here, we present a "fluorescent nanodiamond-electrospun fibrous membrane" strategy, in which a fibrous electrospun cellulose acetate (ECA) membrane replaces the NC membrane and photostable nitrogen-vacancy center nanodiamonds (NVDs) serve as fluorescent labels. The uniform fibrous architecture of the ECA membrane reduces scattering and substrate-derived fluorescence; meanwhile, the fibrous network facilitates smoother convective wash-through, mitigating nonspecific adsorption and mechanical trapping of nanoparticles. As a result, unbound labels are more efficiently removed, leading to suppressed background signals and improved quantitative robustness. Using this platform, we achieved sensitive detection of cardiac troponin I (cTnI) with a limit of detection of ∼0.009 ng/mL, markedly better than conventional NC-based LFA strips. Clinical testing further confirms the diagnostic performance and consistency of the proposed approach. This work offers a simple route to enhance LFA sensitivity and quantification and is readily extendable to other point-of-care biosensing applications.

PMID 42503712
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PubMedToxins2026-07-27

A Comprehensive Chemical-Biological Investigation of the Moderately Toxic Plant Prospero autumnale: Insights into Its Bioactive Potential Using In Vitro and In Vivo Models.

Korichi Maroua M, Smara Ouanissa O, Harchaoui Lilya L, D'Urso Gilda G et al.

Prospero autumnale L. is a Mediterranean medicinal plant traditionally employed for inflammatory and neurological disorders. Nonetheless, its safety profile, toxicity, and application for treating inflammation and pain are yet to be comprehensively established. This investigation aimed to assess the bioactivity and toxicity of extracts derived from its aerial (AgP) and underground (UgP) parts. The phytochemical constituents of various P. autumnale extracts were analyzed using LC-MS/MS, and their phenolic content was quantified. The biological activities were evaluated through in vitro assays-including antioxidant, anti-inflammatory, acetylcholinesterase-inhibitory, and photoprotection assessments-and in vivo experiments, including evaluations of acute oral toxicity, anti-inflammatory, and analgesic effects. UgP extracts demonstrated significant antioxidant activity, with the methanolic extract exhibiting the highest reducing and superoxide scavenging capacities. Dichloromethane and ethyl acetate extracts performed exceptionally well in ABTS and DPPH assays. The aqueous extract from AgP exhibited noteworthy anti-inflammatory and analgesic effects, surpassing diclofenac in vitro and demonstrating efficacy in vivo. It also showed considerable acetylcholinesterase inhibition, while the ethyl acetate extract displayed high photoprotective potential. The acute toxicity was moderate (LD50: 300-400 mg/kg), indicating dose-dependent risks. LC-MS/MS analysis revealed diverse phenolics potentially contributing to both therapeutic and adverse effects. This research enhances the medicinal prospects of P. autumnale, provides new perspectives on plant utilization, and suggests its potential as a natural anti-inflammatory agent. However, due to moderate toxicity and dose-dependent effects, cautious application is advised. These findings underscore the importance of toxicological evaluation alongside bioactivity screening in ethnopharmacology to ensure safety.

PMID 42506705
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