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.
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