Relationship of hydrophobicity and membrane permeability in macrocycles

Encycle Therapeutics是一家加拿大初创公司，该公司使用一种独特的化学平台，由多伦多大学安德烈·尤丁博士的实验室开发，制造一种名为“大环”的新型药物样分子。为了使这些分子成为有效的药物，Encycle需要能够预测当作为药丸口服时，大环是否能被人体吸收。这是至关重要的，因为以药丸形式服用的药物的吸收取决于药物分子穿过小肠膜的能力。虽然在进行药物吸收测量之前，制药公司通常会用利平斯基五定律（Lipinski’s Rule of Five）的一组参数来估计一种药物是否会穿过膜，但使大环如此令人兴奋的潜在药物的独特化学性质也使得使用利平斯基定律来确定它们是否会穿过膜具有挑战性

Encycle Therapeutics is a Canadian start-up company that uses a unique chemistry platform, developed by the laboratory of Dr. Andrei Yudin at the University of Toronto, to make novel, drug-like molecules called macrocycles. For these molecules to become effective drugs, Encycle needs to be able to predict whether or not a macrocycle can be absorbed by the body when taken by mouth as a pill. This is critical because absorption of a drug taken in pill form depends on the ability of the drug molecule to cross the membranes of the small intestine. While companies usually estimate if a drug will cross membranes with a set of parameters called Lipinski's Rule of Five before trying out drug absorption measurements, the unique chemistry that makes macrocycles such exciting potential drugs also makes it challenging to use Lipinski's rules to decide if they will