Octreotide

ctreotide · DARAMONOL · GMP(CFDA) · OXTREOTIDE · Longastatin · Octreotide acetate · Octreotode Acetate · Ocetreotide, Acetate

https://huagongshe.com/ko/chemical/448601

식별자 및 물리적 특성

CAS No.	83150-76-9
분자식	C49H66N10O10S2
평균 분자량	1,019.2 g/mol
단동위원소 질량	1,018.44048031 g/mol
SMILES	C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O
InChIKey	DEQANNDTNATYII-OULOTJBUSA-N
PubChem CID	448601
ChEMBL	CHEMBL1680
DTXSID	DTXSID0048682

화학 및 물리적 성질

XLogP	1
극성 표면적	383
수소 결합 공여자 수	13
수소 결합 수용자 수	14
회전 가능 결합 수	17
무거운 원자 수	71
형식 전하	0
복잡도	1,740
Human Drugs	Breast FeedingLactationMilk, HumanAntineoplastic Agents, HormonalGastrointestinal AgentsEMA approved medicines: Human medicineMedicines for disorders of the pituitary hormone system
녹는점	153-156>140°C (dec.)
끓는 점	1447.2±65.0 °C(Predicted)
밀도	1.39±0.1 g/cm3(Predicted)
저장 조건	-20°C
용해도	아세트산, DMSO 및 메탄올에 용해됨
pKa(산도 계수)	12.60±0.70(Predicted)
물리적 상태	고체
색상	흰색에서 황백색까지
용해도	Soluble to 1.20 mg/ml in water
안정성	흡습성
InChIKey	DEQANNDTNATYII-MEUDYGGUSA-N

안전 및 규제

규제 정보	Octreotide: Does not have an individual approval but may be used under an appropriate group standard
Hepatotoxicity	Mild, transient, asymptomatic elevations in serum aminotransferase levels occur in a small proportion of patients receiving octreotide, and in some individuals the elevations are persistent and worsen over time and may require drug discontinuation. In addition, several instances of acute, clinically apparent liver injury attributable to octreotide have been described. The onset is generally within 1 to 6 months of starting therapy and injury may be more frequent with higher doses. Most cases of liver injury associated with octreotide therapy have been asymptomatic and anicteric, and marked by prominent elevations in serum ALT and AST with normal or near normal serum alkaline phosphatase, GGT and bilirubin. In some instances, however, jaundice has arisen, particularly with rechallenge. There have been no instances of acute liver failure or vanishing bile duct syndrome associated with octreotide, and a characteristic feature of the injury is the rapidity of improvement upon stopping the injections or infusions. Several instances of marked aminotransferase elevations with rapid improvements on stopping have been reported in newborns and infants with congenital hyperinsulinemia who were treated with continuous infusions of high doses of octreotide.
유해 작용	* Gastrointestinal abnormalities (34% to 61%) are transient and usually mild to moderate. They include diarrhea, nausea, abdominal discomfort, gallbladder abnormalities, such as cholelithiasis and microlithiasis, biliary sediment and sludge due to alteration of fat absorption, and possibly by decreasing motility of the gallbladder.
독성 요약	Limited studies have assessed octreotide toxicity. However, isolated studies have shown a mild degree of bone marrow suppression and impairment in spermatogenesis due to inhibition of serum inhibin B and concomitant increase in FSH in supratherapeutic doses. There is a need to conduct significantly larger studies and trials to define and establish the therapeutic index of octreotide and identify its toxic effects and its management.
Drug Induced Liver Injury	Drug-Induced Liver Injury Severity and Toxicity (DILIst)octreotideDILI PositiveIntravenousDOI:10.1016/j.drudis.2019.09.022
Effects During Pregnancy and Lactation	◉ Summary of Use during Lactation

용도

개요

Octreotide is a long-acting somatostatin analog indicated for symptomatic control in acromegaly and gastroenteropancreatic tumors. Other potential uses under investigation include diabetes, psoriasis and Alzheimer's disease.

용도

Octreotide Acetate is the acetate salt of a synthetic long-acting cyclic octapeptide with pharmacologic properties mimicking those of the natural hormone somatostatin. It inhibits the secretion of growth hormone, glucagon, insulin, gastrin, vasoactive intestinal peptide, secretin, motilin and pancreatic polypeptide. Octreotide acetate was uses for the treatment of severe diarrhea and flushing associated with malignant carcinoid tumors, acromegaly, and diarrhea associated with VIPoma; and, then in 2010, for the treatment of neuroendocrine tumors.

일반 설명

Octreotide is a somatostatin analogue with D-Phe-Cys-Phe-D-Trp-Lys-ThrCys-Thr-OH amino acid sequence.