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The following parameters have been estimated for each of 3 different chemotherap

ID: 123671 • Letter: T

Question

The following parameters have been estimated for each of 3 different chemotherapy drugs under consideration for use in chemotherapy wafers (like Gliadel). Based on these values, discuss which compound will achieve the greatest penetration in tissue and which might be expected to have the greatest therapeutic effect.

Property

BCNU

4-HC

Methotrexate

Molecular weight

214

293

454

Log Koil/water

1.53

0.6

-1.85

k (s-1)

0.02

0.02

0.0003

D (10-7 cm2/s)

14

14

5

EC50 in cell culture

25

10

0.04

Property

BCNU

4-HC

Methotrexate

Molecular weight

214

293

454

Log Koil/water

1.53

0.6

-1.85

k (s-1)

0.02

0.02

0.0003

D (10-7 cm2/s)

14

14

5

EC50 in cell culture

25

10

0.04

Explanation / Answer

Your first compound formula is having highest penetration and maximum therapeutic effect that is BCNU because

1. It's molecular weight is less as compared to other so easily passed via cell by active or passive absorption

2. It's partition coefficient is more as compare to other so it is more lipid soluble hence easily pass via cell and have great solubility and high absorption

3. EC 50 is used to check the potency of drug and here it is high as compare to other.