Last update 01 Nov 2024

LIPF

Last update 01 Nov 2024

Basic Info

Synonyms

Gastric lipase, Gastric triacylglycerol lipase, GL

+ [5]

Introduction

Catalyzes the hydrolysis of triacylglycerols to yield free fatty acids, diacylglycerol, monoacylglycerol, and glycerol (PubMed:2243091, PubMed:10358049). Shows a preferential hydrolysis at the sn-3 position of triacylglycerol (PubMed:2243091).

Drugs associated with LIPF

Cetilistat

Target

LIPF

Mechanism

LIPF inhibitors

Active Org.

Takeda Pharmaceutical Co., Ltd.

Originator Org.

Norgine Europe BV

Active Indication

Obesity

Inactive Indication

Type 2 diabetes mellitus in obese

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date20 Sep 2013

Acarbose/Orlistat

Target

LIPF x MGAM

Mechanism

LIPF inhibitors [+1]

Active Org.

Empros Pharma AB

Originator Org.

Empros Pharma AB

Active Indication

Obesity

Inactive Indication-

Drug Highest PhasePhase 2

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Aom-0977 (Hangzhou Adamerck Pharmlabs)

Target

LIPF

Mechanism

LIPF inhibitors

Active Org.-

Originator Org.

Hangzhou Adamerck Pharmlabs, Inc.

Active Indication-

Inactive Indication

Diabetes Mellitus, Type 2 [+1]

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with LIPF

NCT05934110 / Active, not recruitingPhase 2

A 26-week, Double-blind, Randomized Study in Participants With Overweight or Obesity Investigating the Added Contribution of Acarbose in EMP16 on Efficacy, Safety and Tolerability

This is a randomized, double-blind study in participants with overweight or obesity in which the effect of acarbose and the impact of dose on efficacy, safety and tolerability is investigated by comparing the EMP16 combination product with modified release (MR) orlistat, orlistat in its conventional dosage form and placebo.

Start Date18 Apr 2023

Sponsor / Collaborator

Empros Pharma AB

[+1]

NCT04521751 / CompletedPhase 1/2

Lean Efficacy Phase IIa Proof of Concept Trial (LEAAP). A Study in Overweight and Obese Patients During Twenty-six Weeks, Investigating the Effect of EMP16-02 on Body Weight, Safety and Clinical Biomarkers

This study is a proof of concept study to demonstrate that EMP16-02, a fixed dose combination (FDC) of orlistat and acarbose in an oral multiple-unit modified release (MR) formulation leads to a clinically relevant decrease in body weight. The study aims to evaluate the efficacy, safety and tolerability of treatment with two different doses of EMP16 02 (120 mg orlistat/40 mg acarbose and 150 mg orlistat/50 mg acarbose) for 26 weeks on reducing body weight in obese patients.

Start Date07 May 2020

Sponsor / Collaborator

Empros Pharma AB

[+1]

CTRI/2019/11/021919 / Active, not recruitingPhase 3

A Phase III, Multi-Center, Comparative, Randomized, Parallel Group Study to Evaluate the Efficacy and Safety of Cetilistat in Adult Obese Patients

Start Date09 Nov 2019

Sponsor / Collaborator

Hetero Labs Ltd.

100 Clinical Results associated with LIPF

100 Translational Medicine associated with LIPF

0 Patents (Medical) associated with LIPF

271

Literatures (Medical) associated with LIPF

22 May 2024·Bioscience, Biotechnology, and Biochemistry

Human milk-specific fat components enhance the secretion of ghrelin by MGN3-1 cells

Article

Author: Kaneko, Kentaro ; Funatsu, Yui ; Nakamura, Yoshitaka ; Taniguchi, Eriko ; Iwakura, Hiroshi ; Ohinata, Kousaku

AbstractTriacylglycerols (TAGs) are a major fat component in human milk. Since gastric lipase produces 1,2-diacylglycerol from TAGs, we focused on the bioactivity of human milk-derived diacylglycerols in stomach cells. Ghrelin is produced in the stomach and acts as an important regulator of growth hormone secretion and energy homeostasis. In this study, we showed that 1-oleoyl-2-palmitoylglycerol (OP) increased ghrelin secretion, whereas 1,3-dioleoyl-2-palmitoylglycerol (OPO), a major component of human milk TAGs, did not increase ghrelin secretion in the ghrelin-secreting cell line, MGN3-1. Therefore, diacylglycerol OP may directly contribute to the regulation of ghrelin secretion. We also found that 2-palmitoylglycerol and 1- and 2-oleoylglycerol increased ghrelin secretion. Finally, we demonstrated that intracellular cAMP levels and preproghrelin and ghrelin O-acyl transferase expression levels were enhanced by OP treatment in MGN3-1 cells. This may represent an example of a novel mother-infant interaction mediated by fat components derived from human breast milk.

01 Apr 2024·Nutrition in Clinical Practice

Fat digestion and absorption: Normal physiology and pathophysiology of malabsorption, including diagnostic testing

Review

Author: Omer, Endashaw ; Chiodi, Cristina

AbstractFat digestion and absorption play crucial roles in maintaining energy homeostasis and supporting essential physiological functions. The initial stage of fat digestion occurs in the stomach, where gastric lipase begins the hydrolysis of triglycerides. However, most fat digestion takes place in the small intestine via pancreatic enzymes and bile salts. Emulsification of fat by bile acids facilitates enzymatic action, breaking down triglycerides into free fatty acids and monoglycerides, which are then able to be absorbed by enterocytes. Fat malabsorption can result from various underlying conditions, such as exocrine pancreatic insufficiency, bile acid disorders, or intestinal diseases. The clinical manifestations of fat malabsorption include steatorrhea, malnutrition, and deficiencies of fat‐soluble vitamins. Diagnostic approaches involve assessing fecal fat levels, imaging studies, and various functional tests to identify the specific etiology. This review article will describe the normal physiologic process of fat digestion and absorption and discuss various pathophysiology that can lead to fat malabsorption within the gastrointestinal tract as well as their respective diagnostic testing modalities. Effective digestion of fat is essential for overall health, because it allows for absorption of many essential nutrients, plays an integral role in cellular and structural function, and supplies energy to the body. When this is dysfunctional, disorders of malabsorption can occur. This article will give a brief overview of the physiologic process of fat digestion and absorption in healthy individuals as well as review important pathophysiology that can lead to fat malabsorption within the gastrointestinal tract and current diagnostic testing modalities.

01 Feb 2024·International Journal for Vitamin and Nutrition Research

Gastrointestinal genetic reprogramming of vitamin A metabolic pathways in response of Roux-en-Y gastric bypass

Article

Author: de Moura, Eduardo Guimarães Hourneaux ; Fonseca, Danielle C. ; Sampaio, Priscilla ; Marques, Mariane ; Ishida, Robson Kiyoshi ; de Miranda Torrinhas, Raquel Susana Matos ; Passadore, Mariana Doce ; Sakai, Paulo ; Sala, Priscila ; Heymsfield, Steven B. ; Santo, Marco Aurélio ; Corrêa-Giannella, Maria Lúcia ; Barcelos, Samira ; Guarda, Ismael Francisco Mota Siqueira ; Waitzberg, Dan Linetzky ; Ferreira, Beatriz A. M. ; Machado, Natasha Mendonça

Abstract: Roux-en-Y gastric bypass (RYGB) is one of the most performed bariatric surgical techniques. However, RYGB commonly results, as side effects, in nutritional deficiencies. This study aimed to examine changes in the expression of vitamin A pathway encoding genes in the gastrointestinal tract (GI) and to evaluate the potential mechanisms associated with hypovitaminosis A after RYGB. Intestinal biopsies were obtained through double-balloon endoscopy in 20 women with obesity (age 46.9±6.2 years; body mass index [BMI] 46.5±5.3 kg/m2 [mean±SD]) before and three months after RYGB (BMI, 38.2±4.2 kg/m2). Intestinal mucosal gene microarray analyses were performed in samples using a Human GeneChip 1.0 ST array (Affymetrix). Vitamin A intake was assessed from 7-day food records and serum retinol levels were evaluated by electrochemiluminescence immunoassay. Our results showed the following genes with significant downregulation (p≤0.05): LIPF (−0.60), NPC1L1 (−0.71), BCO1 (−0.45), and RBP4 (−0.13) in the duodenum; CD36 (−0.33), and ISX (−0.43) in the jejunum and BCO1 (−0.29) in the ileum. No significant changes in vitamin A intake were found (784±694 retinol equivalents [RE] pre-operative vs. 809±753 RE post-operative [mean±SD]). Although patients were routinely supplemented with 3500 international units IU/day (equivalent to 1050 μg RE/day) of oral retinol palmitate, serum concentrations were lower in the post-operative when compared to pre-operative period (0.35±0.14 μg/L vs. 0.52±0.33 μg/L, respectively – P=0.07), both within the normal range. After RYGB, the simultaneous change in expression of GI genes, may impair carotenoid metabolism in the enterocytes, formation of nascent chylomicrons and transport of retinol, resulting in lower availability of vitamin A.

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