Orlistat

Intestinal Lipase Inhibitor — ALIMENTARY TRACT AND METABOLISM

Key facts

Orlistat is an ofp drug in the Intestinal Lipase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 1999. Its mechanism of action is classified as Lipase Inhibitors. DrugCentral lists 16 molecular targets, including PNLIP, LIPC and LIPG. Recorded indications include Obesity.

• Approval status: ofp (first approved 1999 by the FDA).
• Drug class: Intestinal Lipase Inhibitor.
• Mechanism of action: Lipase Inhibitors.
• Molecular targets: PNLIP, LIPC, LIPG and DAGLA (16 listed in DrugCentral).
• Indications: Obesity.
• ATC code: A08AB01 (Peripherally acting antiobesity products).
• Molecular formula: C29H53NO5; molecular weight 495.75 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Obesity

Contraindications (11)

• Anorexia nervosa
• Bulimia nervosa
• Calcium Oxalate Renal Calculi
• Drug-induced hepatitis
• Hepatic failure
• Hepatic necrosis
• Liver function tests abnormal
• Malabsorption States
• Obstruction of bile duct
• Primary hyperoxaluria
• Vitamin deficiency

Mechanism & targets

• Mechanism of action (MoA): Lipase Inhibitors
• Established pharmacologic class: Intestinal Lipase Inhibitor

Molecular targets (16)

Target	Gene	Action	Activity
Pancreatic triacylglycerol lipase	PNLIP	inhibitor	IC50 8.90
Hepatic triacylglycerol lipase	LIPC	unknown	IC50 8.52
Endothelial lipase	LIPG	unknown	IC50 8.22
Sn1-specific diacylglycerol lipase alpha	DAGLA	unknown	IC50 8.00
Fatty-acid amide hydrolase 1	Faah	unknown	IC50 8.00
Sn1-specific diacylglycerol lipase alpha	Dagla	unknown	IC50 7.70
Abhydrolase domain-containing protein 16A	ABHD16A	unknown	IC50 7.52
Monoacylglycerol lipase ABHD6	ABHD6	unknown	IC50 7.32
Platelet-activating factor acetylhydrolase	PLA2G7	unknown	IC50 7.30
Sn1-specific diacylglycerol lipase beta	DAGLB	unknown	IC50 7.22
Lipoprotein lipase	LPL	unknown	IC50 7.18
Monoacylglycerol lipase ABHD12	ABHD12	unknown	IC50 7.10
Pancreatic triacylglycerol lipase	PNLIP	unknown	IC50 6.66
Cannabinoid receptor 1	CNR1	unknown	Ki 5.60
Fatty acid synthase	FASN	unknown	IC50 5.33
Gastric triacylglycerol lipase	LIPF	inhibitor	—

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1999-04-23	FDA	—	HOFFMANN LA ROCHE

ATC classification

ATC code	Therapeutic hierarchy
A08AB01	ALIMENTARY TRACT AND METABOLISM › ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS › ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS › Peripherally acting antiobesity products

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Steatorrhoea	176.8
Cerebral venous thrombosis	99.8
Cholelithiasis	90.2
Hyperoxaluria	80.3
Nephropathy	79.7
Drug interaction	79.7
Thalamic infarction	71.2
Acute hepatic failure	68.2
Crystal nephropathy	66.8
Rectal discharge	65.7
Abdominal pain	58.8
Rectal haemorrhage	54.5

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Orlistat is on its molecule page.

• Molecular formula: C₂₉H₅₃NO₅
• Molecular weight: 495.75 g/mol
• CAS number: —
• InChIKey: AHLBNYSZXLDEJQ-FWEHEUNISA-N
• PubChem CID: 3034010

CCCCCCCCCCC[C@@H](C[C@@H]1OC(=O)[C@H]1CCCCCC)OC(=O)[C@H](CC(C)C)NC=O

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Orlistat used for?

DrugCentral lists the following indications for Orlistat: Obesity.

How does Orlistat work?

Orlistat is classified as Lipase Inhibitors; its molecular targets in DrugCentral include PNLIP (inhibitor), LIPC, LIPG and DAGLA.

When was Orlistat first approved?

Orlistat was first approved by the FDA in 1999.

What drug class does Orlistat belong to?

Orlistat is in the Intestinal Lipase Inhibitor class.

What is the chemical formula of Orlistat?

Orlistat has the molecular formula C29H53NO5 and a molecular weight of 495.75 g/mol.

Sources

• DrugCentral drug card 1996 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL175247 — compound record and bioactivity
• PubChem CID 3034010 — chemical identifiers
• DrugBank DB01083 — drug record
• FDA UNII 95M8R751W8 — substance identity
• DailyMed: FDA labels for Orlistat — current prescribing information (label search)
• UniProt P16233 (PNLIP) — target protein
• UniProt P11150 (LIPC) — target protein
• UniProt Q9Y5X9 (LIPG) — target protein
• UniProt Q9Y4D2 (DAGLA) — target protein
• UniProt O95870 (ABHD16A) — target protein
• UniProt Q9BV23 (ABHD6) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.