Delving into the Latest Updates on Cetilistat with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Cametor, Cetilistat (JAN/USAN/INN)

+ [2]

Target

LIPF

Mechanism

LIPF inhibitors(Gastric lipase inhibitors)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Obesity

Inactive Indication

Type 2 diabetes mellitus in obese

Originator Organization

Norgine Europe BV

Active Organization

Takeda Pharmaceutical Co., Ltd.

Inactive Organization

Alizyme Plc

BIOVIA, Inc.

Norgine BV

Drug Highest PhaseApproved

First Approval Date

JP (20 Sep 2013),

Obesity

Regulation-

Login to view timeline

Structure

Molecular FormulaC25H39NO3

InChIKeyMVCQKIKWYUURMU-UHFFFAOYSA-N

CAS Registry282526-98-1

Cafeteria diet (CD) model for in-vivo studies mimics the western diet having imbalanced nutritional value, high caloric-density and palatability. Uncontrolled eating leads to the development of childhood obesity, poor self-esteem and depression due to its effects on brain development. Herbal supplements are novel inclusion in the management of obesity and mental well-being. Pterostilbene (PTE) found in blueberries and Pterocarpus marsupium heartwood, is known to prevent obesity in invivo models. Adolescent Swiss albino male mice were fed on CD for 70 days and the development of obesity was assessed by gain in body weight, abdominal circumference. Forced swim and tail suspension test confirmed depression in CD fed mice. Obesity induced depressed (OID) mice were treated with PTE (10, 20, 40 mg/kg), standard antiobesity drug cetilistat (10 mg/kg), antidepressant fluoxetine (10 mg/kg) for 28 days. Post treatment, PTE-treated mice showed reduction in BW and depression-like behavior analysed using paradigms such as sucrose preference, open field, marble burying, and resident intruder test in comparison to the CD group. Insulin resistance, lipid profile, antioxidant enzyme, inflammatory cytokines (NF-κB, IL-6, TNF α) and cortisol levels were mitigated by PTE. It also restored normal cellular architecture of the brain and adipose tissue and increased the Silent mating type information regulation 2 homolog1 (SIRT1), leptin and ghrelin receptors gene expression in the brain. Thus, it can be concluded that PTE might have inhibited OID like behavior in mice via inhibition of IR, modulating neuroinflammation and hypothalamic-pituitary-adrenal axis dysfunction and upregulating SIRT1 mediated leptin-ghrelin signaling.

30 Mar 2023·Scientific reports

Metabolic profiling, antioxidant, and enzyme inhibition potential of Iris pseudacorus L. from Egypt and Japan: A comparative study.

Article

Author: Ayoub, Iriny M ; Devkota, Hari Prasad ; Singab, Abdel Nasser B ; Watanabe, Masato ; Yehia, Suzan M

Genus Iris comprises numerous and diverse phytoconstituents displaying marked biological activities. The rhizomes, and aerial parts of Iris pseudacorus L. cultivars from Egypt and Japan were subjected to comparative metabolic profiling using UPLC-ESI-MS/MS. The antioxidant capacity was determined using DPPH assay. In vitro enzyme inhibition potential against α-glucosidase, tyrosinase and lipase was evaluated. In silico molecular docking was conducted on the active sites of human α-glucosidase and human pancreatic lipase. Forty-three compounds were tentatively identified including flavonoids, isoflavonoids, phenolics and xanthones. I. pseudacorus rhizomes extracts (IPR-J and IPR-E) exhibited the highest radical scavenging activity with IC₅₀ values of 40.89 µg/mL and 97.97 µg/mL, respectively (Trolox IC₅₀ value was 14.59 µg/mL). Moreover, IPR-J and IPR-E exhibited promising α-glucosidase inhibitory activity displaying IC₅₀ values of 18.52 µg/mL, 57.89 µg/mL, respectively being more potent as compared to acarbose with IC₅₀ value of 362.088 µg/mL. All extracts exerted significant lipase inhibitory activity exhibiting IC₅₀ values of 2.35, 4.81, 2.22 and 0.42 µg/mL, respectively compared to cetilistat with IC₅₀ value of 7.47 µg/mL. However, no tyrosinase inhibitory activity was observed for all I. pseudacorus extracts up to 500 µg/mL. In silico molecular modelling revealed that quercetin, galloyl glucose, and irilin D exhibited the highest fitting scores within the active sites of human α-glucosidase and pancreatic lipase. ADMET prediction (absorption, distribution, metabolism, excretion, and toxicity) showed that most of the phytoconstituents exhibited promising pharmacokinetic, pharmacodynamics and tolerable toxicity properties. According to our findings, I. pseudacorus might be considered as a valuable source for designing novel phytopharmaceuticals.

01 Jan 2023·Informatics in Medicine Unlocked

Repurposing FDA-approved drugs cetilistat, abiraterone, diiodohydroxyquinoline, bexarotene, and remdesivir as potential inhibitors against RNA dependent RNA polymerase of SARS-CoV-2: A comparative in silico perspective

Article

Author: Khademi, Fatemeh ; Shahabadi, Nahid ; Zendehcheshm, Saba ; Mahdavi, Mohammad

Vaccines are undoubtedly the most effective means of combating viral diseases like COVID-19. However, there are risks associated with vaccination, such as incomplete viral deactivation or potential adverse effects in humans. However, designing and developing a panel of new drug molecules is always encouraged. In an emergency, drug repurposing research is one of the most potent and rapid options. RdRp (RNA-dependent RNA polymerase) has been discovered to play a pivotal role in viral replication. In this study, FDA-approved drugs bexarotene, diiodohydroxyquinoline, abiraterone, cetilistat, and remdesivir were repurposed against the RdRp by molecular modeling, docking, and dynamic simulation. Furthermore, to validate the potency of these drugs, we compared them to the antiviral remdesivir, which inhibits RdRp. Our finding indicated that the selected drugs have a high potential to be developed as RdRp inhibitors and, with further validation studies, could serve as potential drugs for the treatment of COVID-19.

100 Deals associated with Cetilistat

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D09208	Cetilistat	A08A	DB06586

R&D Status

Approved

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Obesity	JP	Takeda Pharmaceutical Co., Ltd.	20 Sep 2013

Developing

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Type 2 diabetes mellitus in obese	Phase 3	GB	Alizyme Plc	01 Dec 2004
Type 2 diabetes mellitus in obese	Phase 3	SE	Alizyme Plc	01 Dec 2004
Type 2 diabetes mellitus in obese	Phase 3	FI	Alizyme Plc	01 Dec 2004
Obesity	Preclinical	-	Norgine BV	20 Sep 2013
Obesity	Discovery	-	Norgine BV	20 Sep 2013
Type 2 diabetes mellitus in obese	Discovery	NL	Alizyme Plc	01 Dec 2004
Type 2 diabetes mellitus in obese	Discovery	DK	Alizyme Plc	01 Dec 2004

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00156897 (Pubmed \| Obesity (Silver Spring))	Phase 2	Obesity	-	Cetilistat 40 mg	(bundkiqfxb) = xwkapvqrob kisosqmjbe (ytfeywobpv )	-	01 Jan 2010
				Cetilistat 80 mg	(bundkiqfxb) = begncahkfr kisosqmjbe (ytfeywobpv )