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octreotide acetate (OOA / oral octreotide / Octreolin)

✓ Approved

Chiasma, Inc. · SSTR2 · Small Molecule

What is octreotide acetate?

octreotide acetate is a small molecule developed by Chiasma, Inc.. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesOOA, oral octreotide, Octreolin
CompanyChiasma, Inc.
Drug ClassSmall Molecule, Polypeptide
Molecular TargetSSTR2, SSTR5
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Chiasma, Inc.

Mechanism of Action

Molecular Targets

octreotide acetate acts on 2 molecular targets:

SSTR2somatostatin receptor 2 (SST2)
SSTR5somatostatin receptor 5 (SST5, SS-5-R)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

octreotide acetate is developed for 6 unique indications across 4 therapeutic areas.

Therapeutic AreaConditionPhase
Endocrine disordersAcromegaly✓ Approved
Endocrine disordersCarcinoid syndromePhase II
Hepatobiliary disordersPortal hypertensionPhase II
Vascular disordersHypertensionPhase I
Gastrointestinal disordersPancreatitisPhase I

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Related Research Articles

PubMedJournal of complementary & integrative medicine2026-09-19

In vitro, in vivo, and computational evaluation of xanthine oxidase inhibitory and antihyperuricemic activities of Piper betle L. ethyl acetate fraction.

Hao Bui Thi BT, Minh Phan Hong PH, Anh Hong Nguyen Thi NT, Nhat Hoang Nam HN et al.

Gout is a metabolic disorder characterized by hyperuricemia and urate crystal deposition. This study evaluated the xanthine oxidase inhibitory, antihyperuricemic, anti-inflammatory, analgesic, and in silico target-binding properties of an EtOAc fraction of Piper betle L. aerial parts. P. betle aerial parts were extracted with ethanol and partitioned to obtain an EtOAc fraction. Xanthine oxidase inhibition was evaluated spectrophotometrically, and antihyperuricemic activity was examined in potassium oxonate-treated mice given the fraction (200 or 600 mg/kg). Carrageenan-induced paw edema and acetic acid-induced writhing were used to assess anti-inflammatory and analgesic effects. Hydroxychavicol was docked with xanthine oxidase, cyclooxygenase-2, and transient receptor potential vanilloid 1, followed by molecular dynamics simulations. The ethyl acetate fraction inhibited xanthine oxidase with an IC50 of 4.28 ± 0.15 μg/mL, whereas allopurinol showed an IC50 of 1.06 ± 0.07 μg/mL. In hyperuricemic mice, serum uric acid showed a decreasing trend, and urinary uric acid was significantly reduced at 600 mg/kg. Paw edema was reduced at 600 mg/kg, whereas writhing responses were not significantly inhibited. Docking predicted favorable hydroxychavicol binding to the three targets, but molecular dynamics indicated weaker ligand retention in the xanthine oxidase complex than in the cyclooxygenase-2 and transient receptor potential vanilloid 1 complexes. The ethyl acetate fraction of P. betle demonstrated preclinical xanthine oxidase inhibitory, urate-lowering, and anti-inflammatory potential. Stronger chemical standardization and mechanistic validation are required before therapeutic relevance can be inferred.

PMID 42762091
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PubMedFood chemistry: X2026-09-19

Key aroma contributors and perceptual interactions of dried longan-like aroma in lapsang souchong black tea with different natural aging times.

Shi Yutao Y, Zuo Lirong L, Huang Canyang C, Zhou Yanhua Y et al.

This study investigated aroma evolution in Lapsang Souchong black tea (LS) with different natural aging times and the perceptual basis of its dried longan-like aroma. Sensory evaluation, HS-SPME-GC-MS, aroma recombination/omission, S-curve-Feller analysis, and molecular simulations showed that, with increasing natural aging time, LS aroma shifted from pine-smoke, sweet, and fruity aroma dominance to prominent dried longan-like aroma, followed by enhanced woody and aged aromas. LS19 showed the highest dried longan-like aroma intensity. Benzaldehyde, Geranyl acetate, and 2-Acetylfuran were identified as key contributors. Binary mixtures mainly showed additive effects, whereas the ternary system exhibited a synergistic effect. Molecular simulations suggested stable binding of the key aroma compounds with the candidate olfactory receptor OR1A1 (-53.89 kcal/mol), with ILE126 and VAL227 identified as key binding residues. These findings clarify the material basis and perceptual features of dried longan-like aroma and support LS quality evaluation, storage management, and aroma regulation.

PMID 42761899
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PubMedResearch in veterinary science2026-09-19

Melatonin testicular synthesis and its role in reproductive physiology in seasonal and non-seasonal breeders.

Cesauri Mattia M, Ventrella Domenico D, Fanelli Diana D, Elmi Alberto A

Melatonin (MT) is an indoleamine primarily produced by the pineal gland in a light-dark-dependent manner; however, it is also locally synthesized in the testis, where it influences male reproductive physiology upon interaction with its receptors (MT1/MT2), the binding started the bio-signaling inside the cells mediated by MT. This review outlines the intratesticular effects of MT, addressing seasonal and non-seasonal mammals. In rodents, Leydig, Sertoli, and germ cells contain enzymatic machinery to produce MT, with MT1/MT2 signaling influencing androgen production through cAMP-dependent and independent pathways and interacting with local Corticotropin-Releasing Hormone (CRH), serotoninergic, and catecholaminergic systems to regulate steroidogenesis and testicular plasticity. In non-seasonal species, Sertoli cells express MT1/MT2 and react to melatonin through alterations in proliferation, expression of spermatogenesis-related genes, and restructuring of glycolytic and acetate metabolism, thus modifying energetic support to germ cells. In seasonal breeders like rams and roe deer, MT1/MT2, N-acetyltransferase (AANAT), and acetylserotonin O-methyltransferase (ASMT) are found in testicular cells, spermatozoa, and the epididymis. Exogenous MT treatments are linked to advancements in the breeding season, increased testicular size and enhanced testosterone secretion in rams. MT1/MT2 were reported in spermatozoa from several seasonal and non-seasonal mammalian species and MT frequently was detected in seminal plasma, where they are involved in motility, capacitation, cryotolerance, and antioxidant protection. Therefore, suggesting that MT serves as a conserved but diversified intratesticular signal that integrates photoperiodic, metabolic, and cytoprotective regulation of male fertility.

PMID 42762694
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PubMedInorganic chemistry frontiers2026-09-19

Design of bifunctional pyridinophane ligands as Mn2+ MRI agents for diagnostic imaging of Alzheimer's disease.

El Sayed Tarek T, Patel Akhil A, Xu Kerui K, Salaiza Jennifer A JA et al.

Alzheimer's disease (AD) is a progressive neurodegenerative disorder whose prevalence is rising with the aging of the global population. Among the proposed pathological hallmarks, the beta-amyloid (Aβ) peptide aggregates and soluble Aβ oligomers are established biomarkers and remain valuable diagnostic targets. While positron emission tomography (PET) imaging agents dominate AD diagnostic imaging, there are no FDA-approved MRI agents for AD. Herein, we report five bifunctional chelators built on the 2,11-diaza[3.3](2,6)pyridinophane framework, and which were evaluated as chelators for Mn2+-based MRI contrast agents. Based on in vitro studies, including thermodynamic stability and kinetic inertness measurements, T 1 relaxivity and 17O transverse relaxivity measurements to extract hydration numbers and water-exchange parameters, we obtained a clear structure-activity correlation for the corresponding bifunctional chelators: anionic picolinate and acetate arms increase thermodynamic stability and kinetic inertness, while the benzothiazolyl-phenol arm accelerates water exchange. Importantly, a high hydration number alone is insufficient, as a rapid water exchange is also needed for an appreciable contrast. Moreover, we show both the bifunctional chelators and their Mn2+ complexes exhibit appreciable affinity for Aβ aggregates, both in vitro and in 5xFAD mouse brain sections. [Mn(TE-8)], the most kinetically inert complex with favorable relaxivity, log D, and Aβ affinity, was advanced to in vivo MRI studies. Unlike MnCl2, which accumulates non-specifically, [Mn(TE-8)] cleared through renal and hepatobiliary routes and produced measurable brain contrast enhancement. Together, these results establish the diazapyridinophane scaffold as a viable first-generation platform for blood-brain barrier (BBB)-permeable Mn2+ MRI contrast agents.

PMID 42761867
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PubMedAnalytica chimica acta2026-09-19

Surfactant deep eutectic solvents for extraction and HPLC-PDA analysis of antipsoriatic drugs in spiked water and lipophilic topical matrices.

Alamir Samy G SG, Magdy Nancy N, Ibrahim Adel Ehab AE, Hussein Lobna A LA et al.

Deep eutectic solvents (DESs) have garnered attention in various disciplines due to their unique properties. In this work, different surfactants were screened as hydrogen-bond acceptors in combination with structurally related phenols as hydrogen-bond donors (HBDs), and successful and unsuccessful pairings were discussed. Literature on successfully paired surfactants was also reviewed. Nevertheless, the screening results and reported classifications, together with the observed aqueous behavior and variable extraction performance across different matrices, prompted further investigation of composition-behavior relationships of these systems. Five surfactant-phenolic DESs were synthesized by mixing o-cresol (CRS) or catechol with dodecyltrimethylammonium bromide (DTAB), cetyltrimethylammonium bromide (CTAB), or Brij35 at 75.0 °C for 30.0 min. Although more hydrophobic HBDs were used than in previous studies, the resulting DESs displayed transient aqueous dispersion after vortexing and subsequently re-separated on standing. Their viscosity (64.21-1389 mPa s) and conductivity (1.00-447.00 μS/cm) also varied. 1H/13C nuclear magnetic resonance and Fourier-transform infrared spectroscopy indicated hydrogen bonding between phenolic hydroxyl groups and bromide/ether acceptors, with features suggesting π-cation association in cationic-surfactant systems. To probe their practicality, a high-performance liquid chromatography method with photodiode array detection was developed for betamethasone valerate, halobetasol propionate, fusidic acid, and tazarotene, achieving separation within 6 min, and compared with five reported chromatographic methods. Validation per the International Council for Harmonisation Q2 (R1) guidelines demonstrated linearity (R2 0.9997-0.9999), accuracy (98.2-102.4%), and precision (≤2.0%), with robustness evaluated through experimental design. Brij35-based systems showed reduced extraction recoveries for lipophilic topical formulations. After additional screening, CRSCTAB and CRSDTAB DESs were used with spiked water samples as a hydrophilic proof-of-concept matrix, employing salting-out-assisted liquid-liquid microextraction using ammonium acetate. The results suggest provisional amphiphilic-like rather than conventional hydrophobic-DES behavior; however, thermal phase diagrams, equilibrium water-solubility measurements, and broader thermodynamic investigations remain necessary before any formal reclassification.

PMID 42763156
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PubMedZhong nan da xue xue bao. Yi xue ban = Journal of Central South University. Medical sciences2026-09-19

Plasmid-encoded Pgp3 protein enhances the infectivity of Chlamydia trachomatis serovar L2 in mice.

Sun Xin X, Zhang Qi Q, Tian Qi Q, Xue Min M et al.

Chlamydial infection can cause a variety of serious diseases, including trachoma, tubal infertility, and rectal lymphogranuloma venereum (LGV). However, the underlying pathogenic mechanisms remain incompletely understood. Chlamydia trachomatis (C. trachomatis) serovar L2 was among the first chlamydial strains to be successfully transformed and has been widely used to investigate the functions of chlamydial proteins, particularly plasmid-encoded proteins. Previous studies of serovar L2 have largely been limited to in vitro experiments, and the roles of plasmid-encoded proteins during in vivo infection remain poorly understood. This study aims to evaluate the infectivity in mice of L2 mutants carrying deletions or premature stop codon mutations in different plasmid genes. Female C3H/HeJ and CBA/J mice received a subcutaneous injection of medroxyprogesterone acetate 5 days before infection and were subsequently inoculated intravaginally or intrauterinely with 1.0×106 inclusion-forming units (IFUs) of various L2 strains. These included wild-type L2 (L2wt), plasmid-free L2 (L2R), green fluorescent protein (GFP)-expressing L2 (L2GFP), plasmid-encoded glycoprotein (Pgp)-related deletion mutants (L2ΔPgp3, L2ΔPgp4, L2ΔPgp5, and L2ΔPgp7), and premature stop-codon mutants (L2Pgp3Y9S, L2Pgp4K13S, L2Pgp5L9S, L2Pgp7L11S, and L2Pgp8E11S). Vaginal swabs were collected at regular intervals after infection, and viable chlamydial shedding was monitored by immunofluorescence-based titration. The infectivity of each mutant was compared with that of the L2wt or L2GFP control group. For in vitro experiments, HeLa cells infected with the above strains were harvested at 30 or 48 h post-infection. Immunofluorescence staining and Western blotting (WB) were performed to assess the expression levels of Pgp3 and glycogen synthase A (GlgA), respectively. Compared with L2wt, the plasmid-free strain showed significantly reduced chlamydial shedding after intrauterine infection (P<0.05), whereas no such difference was observed after intravaginal infection, suggesting that the L2 plasmid plays a more important role in upper genital tract infection than in lower genital tract infection. Deletion of either Pgp3 (L2ΔPgp3) or Pgp4 (L2ΔPgp4) resulted in significantly reduced vaginal shedding of viable chlamydia after intrauterine inoculation (P<0.05). Mice infected with the Pgp3 premature stop codon mutant L2Pgp3Y9S exhibited reduced shedding (P<0.05), whereas this phenotype was not observed with the Pgp4 mutant L2Pgp4K13S. Immunofluorescence staining and WB showed that L2Pgp4K13S still expressed a detectable amount of Pgp3, although markedly less than L2wt, and this residual expression may have been sufficient to maintain infectivity. WB further confirmed that expression of the C. trachomatis glycogen synthase GlgA depends on Pgp4 rather than Pgp3. The infectivity of the Pgp4-deficient strain L2Pgp4K13S was comparable to that of L2wt, suggesting that GlgA may not be required for L2 infection of the murine upper genital tract. Pgp3 rather than Pgp4, other plasmid-encoded genes, or the plasmid-regulated GlgA gene, plays a critical role in the infectivity of C. trachomatis serovar L2 in mice. In addition, even very low levels of Pgp3 expression may be sufficient to maintain L2 infectivity in mice.

PMID 42763292
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