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DRUG DISCOVERY TECHNOLOGY OF PREVACID (LANSOPRAZOLE)
HARDIKKUMAR PATEL
21051413
Lansoprazole
- Lansoprazole is a proton pump inhibitor (PPI) and a potent inhibitor of gastric acidity which is widely used in the therapy of gastroesophageal reflux and peptic ulcer disease.
- Lansoprazole was first developed at Takeda and given the development name AG 1749. It is now sold under the brand name prevacid. It was patented by Takeda in 1984, and the medication debuted in 1991. It received medicinal use approval in the US in 1995.
- Dexlansoprazole and levolansoprazole are mixed in a 1:1 racemic mixture. Due to the enantiomeric shift, dexlansoprazole is an active component of a commercial medication that is enantiomerically pure.
Introduction
Lipinski’s ‘Rule of 5’
- Molecular Weight – 369.4 gm/mol. (<500)
- cLogP – 2.8
- No of H bond donor – 1 (<5)
- No of H bond Accepter – 8 (<10)
Properties
2-[[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methylsulfinyl]-1H-benzimidazole
(Source: Chemdraw)
HOW DOES IT WORK?
- Lansoprazole is a prodrug which requires protonation via an acidic environment to get activated.
- Lansoprazol covalently binds with cystien residues specifically Cys813 and Cys321 via disulfide bridges on the subunit of H+/K+ ATPase enzyme system.
- Thereby it inhibits the H+/K+ ATPase pump which in turn inhibits the gastric acid secretion or formation of hydrochloric acid in parietal cells
Target Identification & Validation
(Source:https://www.youtube.com/watch?v=-7xxSojdFfM)
Target identification and validation
Target:
- “ H+,K+, ATPase pumps” receptor on parietal cell in stomach.
Target Validation:
- Prior to the discovery of Lansoprazole, much scientific literature had been published illustrating the role of the proton pump inhibitors in generating acid in the stomach. In vitro experiments were also performed to validate the fact that inhibiting the proton pumps could lead to decrease of acid generation.
Target
(Source: https://slideplayer.com/slide/12932338/)
Lead Compound Generation & Optimization
HTS
Chemical
Library
For Inibition of proton pump
Lead Compound
(Source: Chemdraw)
Discovery Timeline
Timeline
YEAR
Timeline
Topic 4
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