Stability of compounds in new drugs. Refer to the Pfizer Global Research and Develop...

Stability of compounds in new drugs. Refer to the Pfizer Global Research and Development study (reported in ACS Medicinal Chemistry Letters, Vol. 1, 2010) of the metabolic stability of drugs, Exercise 2.35 (p. 49). Recall that the stability of each of 416 drugs was measured by the fup/ fumic ratio.

a. In Exercise 2.35, you determined the proportion of fup/fumic ratios that fall above 1. Use this proportion to determine the percentile rank of 1.

b. In Exercise 2.35, you determined the proportion of fup/fumic ratios that fall below .4. Use this proportion to determine the percentile rank of .4.

Reference: Exercise 2.35

Stability of compounds in new drugs. Testing the metabolic stability of compounds used in drugs is the cornerstone of new drug discovery. Two important values computed from the testing phase are the fraction of compound unbound to plasma (fup) and the fraction of compound unbound to microsomes (fumic). A key formula for assessing stability assumes that the fup/fumic