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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)
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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 chromatography. A2026-08-30

Automated miniaturized LLE-GC-MS/MS for the analysis of EPA 8270 SVOCs and multi-class pesticides in water using ethyl acetate.

Feo Maria Luisa ML, Benedetti Paolo P, Zanaboni Moira M, Tofful Luca L et al.

The determination of trace-level semi-volatile organic compounds (SVOCs) following EPA Method 8270 traditionally relies on manual liquid-liquid extraction (LLE) using large volumes of dichloromethane (DCM). However, recent 2024 TSCA regulations restricting DCM due to human health risks necessitate sustainable analytical alternatives. This study presents a fully automated, miniaturized LLE (micro-LLE) method for 170 analytes including EPA 8270 targets and multi-class pesticides (organochlorine (OCPs), organophosphorus (OPPs) and organonitrogen (ONPs) pesticides and pyrethroids). The workflow utilizes a TriPlus RSH SMART autosampler to integrate standard preparation, surrogate spiking, and extraction with on-line GC-MS/MS injection. Ethyl acetate was validated as a "green" alternative to DCM, with a 1:1 NaCl:MgSO₄ salt mixture optimizing the salting-out effect. This procedure achieved a tenfold enrichment factor using only 1.5 mL of solvent for 10 mL of sample. Method validation showed excellent linearity (R2> 0.995 for 70% of analytes) and precision (RSD < 15%). Method limits of quantification (MLOQs) between 0.05 and 10 µg/L meet stringent regulatory requirements. The method's robustness was confirmed through real-world Saharan deposition samples, identifying high levels of Phenothrin (211 ppb) and Endosulfan ether (140 ppb). This robotic workflow provides a high-throughput, sustainable solution for modern environmental monitoring.

PMID 42669230
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PubMedJournal of nutritional science and vitaminology2026-08-30

Bio-Guided Fractionation of Cardamom Ethyl Acetate Fraction Promotes Glucose Uptake via GLUT4 Translocation through Insulin Signaling Pathway in the Skeletal Muscle.

Fang Liyuan L, Hironao Ken-Yu KY, Ashida Hitoshi H, Yamashita Yoko Y

Regulation of skeletal muscle glucose uptake is an effective strategy for reducing postprandial hyperglycemia and improving whole-body glucose homeostasis in the management of type 2 diabetes. The present study investigated that cardamom enhances glucose uptake in skeletal muscle in vitro and improves glucose tolerance in vivo. Bioactivity-guided fractionation of cardamom identified an ethyl acetate fraction (Fr. A) and its subfraction (Fr. A-i) as potent stimulators of glucose uptake in L6 myotubes. Both fractions significantly promoted glucose uptake by enhancing glucose transporter type 4 (GLUT4) translocation to the plasma membrane. Mechanistic investigations revealed activation of the phosphoinositide 3-kinase (PI3K)/protein kinase B (AKT) signaling pathway, accompanied by increased phosphorylation of Akt substrate of 160 kDa (AS160), a key regulator of GLUT4 vesicle trafficking, while no significant changes were observed in insulin receptor substrate-1 (IRS-1) or AMP-activated protein kinase (AMPK) phosphorylation. Fr. A induced a more pronounced effect on AS160 phosphorylation and was therefore selected for further evaluation. The antihyperglycemic potential of Fr. A was assessed in ICR mice using an oral glucose tolerance test. Oral administration of Fr. A (1 and 10 mg/kg body weight) significantly improved glucose tolerance and alleviated postprandial hyperglycemia. Cardamom in skeletal muscle and highlights its potential as a natural therapeutic candidate for the management of postprandial hyperglycemia.

PMID 42669532
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PubMedBioresource technology2026-08-30

Efficient light-driven CO2 conversion to ethanol using a CQDs/InP@bacteria biohybrid system.

Wang Jiale J, Liu Hao H, Huang Yun Y, Zhu Xianqing X et al.

Bacteria can convert CO2 into acetate and ethanol via the Wood-Ljungdahl pathway with H2 as an electron donor, providing a green route for renewable energy production. However, the low solubility of H2 in water limits conversion efficiency. Although in semi-artificial biohybrid systems such as InP-based systems, photogenerated electrons can replace H2 as an alternative driving force, rapid electron-hole recombination limits carbon fixation efficiency. In this work, CQDs were introduced to construct a CQDs/InP composite to facilitate carrier separation and interfacial electron transfer, forming a CQDs/InP@bacteria biohybrid system. Compared with pure InP, CQDs/InP showed a 78.3% reduction in interfacial charge transfer resistance and a 1.95-fold increase in photocurrent. Metabolomic analysis further revealed that key intermediates involved in intracellular respiration and ATP synthesis, such as succinic acid and fructose 1,6-bisphosphate, were downregulated by 23% and 21.35%, respectively, indicating that the input of external electrons enabled the biohybrid system to effectively reduce the bacterial dependence on intracellular catabolic energy production. Consequently, the CQDs/InP@bacteria biohybrid system under 450 nm blue light achieved acetate and ethanol production of 0.70 and 0.24 g·L-1, respectively, representing increases of 114.46% and 126.98% over the pure bacterial system, with an apparent quantum yield of 1.76%, indicating improved light-to-chemical energy conversion efficiency. This work effectively enhances interfacial electron transfer in InP-based systems and promotes light-driven CO2 fixation and chemical production in non-photosynthetic bacteria, providing a pathway for constructing efficient semi-artificial photosynthetic microbial CO2 conversion systems.

PMID 42669366
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PubMediScience2026-08-30

Intrinsic anti-tumorigenic properties of the skin epithelium promote cancer resistance in naked mole-rats.

Fatima Iqra I, Mardaryev Andrei N AN, Rozhkova Elena E, Botchkareva Natalia V NV et al.

Naked mole-rats (NMRs) are unique long-lived mammals that possess marked resistance to cancer including lack of any reported spontaneous skin cancer incidences. Here, we show that in comparison with mice, homeostatic epidermal keratinocytes in NMRs exhibit elevated expression of 324 tumor suppressor genes of different classes including 55 genes regulating DNA damage/repair. Furthermore, NMR skin grafted onto nude mice exhibits complete resistance to 7,12-dimethylbenz[a]-anthracene/12-O-tetradecanoylphorbol-13-acetate (DMBA/TPA)-induced skin carcinogenesis in tissue-autonomous manner. In contrast to mice, DNA-damaged cells are effectively eliminated from DMBA/TPA-treated NMR epidermis, which exhibits a unique transcription response to DMBA/TPA characterized by high expression of anti-cancer genes, activation of ferroptosis, as well as by downregulation of 80 oncogenes including components of NF-kB, Wnt, and tyrosine kinase receptor signaling pathways. Thus, intrinsic multi-level anti-cancer protective program in NMR epithelial cells serves as unique model for further analyses of natural anti-cancer defense mechanisms and their translation to humans.

PMID 42668625
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PubMedJournal of chromatography. B, Analytical technologies in the biomedical and life sciences2026-08-30

Development and ICH M10-compliant validation of an LC-MS/MS method for quantification of atirmociclib in mouse plasma and its application to preclinical pharmacokinetic studies.

Gaur Ashwani A, Patel Urvesh U, Gavali Ashutosh A, Sekar Sasikumar S et al.

Atirmociclib is a selective cyclin-dependent kinase 4 (CDK4) inhibitor currently under clinical investigation for the treatment of advanced malignancies, particularly hormone receptor positive (HR+) or human epidermal growth factor receptor 2 negative (HER2-) breast cancer. Here, we report the first validated liquid chromatography tandem mass spectrometry (LC-MS/MS) bioanalytical method for the quantification of atirmociclib in mouse plasma, validated in compliance with international council for harmonisation-M10 (ICH-M10) guidelines. Sample preparation involved a rapid and straightforward protein precipitation approach using acetonitrile, yielding consistent recovery (>80%) across low to high concentration levels. Chromatographic separation was achieved on a Kinetex C18 column (50 mm length × 2.1 mm internal diameter, 5 μm particle size) using gradient elution with 5 mM ammonium acetate in water (mobile phase A) and 0.1% v/v formic acid in acetonitrile (mobile phase B). The analyte (atirmociclib) and internal standard (warfarin) were detected using Q1/Q3 (m/z) mass transitions 464.2/303.9 and 309.0/163.0 respectively. The method demonstrated excellent selectivity, accuracy, precision, and linearity over a concentration range of 1-1000 ng/mL. Additionally, reliable quantification was maintained for samples exceeding the upper limit of quantification following up to 10-fold dilution. All validation parameters, including stability in biological matrices and solution, met the predefined acceptance criteria. This sensitive, and reproducible method was successfully applied to support preclinical pharmacokinetic study of atirmociclib in mouse, providing a valuable analytical tool.

PMID 42669270
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PubMedPreventive nutrition and food science2026-08-29

Antioxidant Activity of Heated Radish (Raphanus sativus L.) and Tyrosinase Inhibition.

Jo Yeon Jae YJ, Jung Yun Jo YJ, Yoo Dan Hee DH, Lee In Chul IC et al.

This study evaluated the antioxidant activity and tyrosinase inhibitory effects of heated radish (Raphanus sativus L.). The ethyl acetate fraction of the heated extracts markedly increased total polyphenol content and antioxidant activity. It also strongly suppressed tyrosinase and melanin biosynthesis, without exerting toxicity in B16F10 melanoma cells. It effectively suppressed the levels of key melanogenesis-related proteins, including microphthalmia-associated transcription factor (52.59%), tyrosinase (38.32%), tyrosinase-related protein (TRP)-1 (45.93%), and TRP-2 (50.26%). A series of chromatographic and spectroscopic analyses identified 2,3-dihydro-3,5-dihydroxy-6-methyl-4H-pyran-4-one as the major bioactive compound. It was characterized as a Maillard reaction product of the interactions between sugars and amino acids during heating, notably inhibiting tyrosinase. These results indicate that the ethyl acetate fraction of heated radishes holds potential as a natural ingredient in functional foods with anti-melanogenic activity.

PMID 42666907
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