Soft drug design:inactive & active metabolite based soft drug

1. SOFT DRUG DESIGN:INACTIVE &ACTIVE
METABOLITE BASED SOFT DRUG
Presented by:Farhan Afridi
Roll:1157
Registration No:1160
Department of Pharmacy,University of
Science and Technology Chittagong

2. CONTENTS
Introduction
What are the goals of designing soft drugs?
Inactivate Metabolite-based Soft Drug
Active Metabolite-based Soft Drug
Clinical Success Stories
Future Perspectives
Conclusion

3. Introduction
Soft drugs are active isosteric–isoelectronic analogues of a
lead compound that are deactivated in a predictable and
controllable way after achieving their therapeutic role.
The resultant metabolites formed after deactivation must
have no intrinsic activity of their own,in addition to be non-
toxic to the host.

4. What are the goals of designing
soft drug?
- To develop drug with less or no side effects.
- To avoid non localized and long term toxicity.
- To improve therapeutic index.

5. Inactive metabolite-based soft drugs
Activativation stage: It involves specific chemical modifications of
the inactive metabolite.
Predictable Metabolism:The new structures are designed so that their
metabolism yields the starting inactive metabolite in one step
(metabolic inactivation) without any other metabolic conversions.
Controllable metabolism:The specific binding and transport
properties,as well as the metabolic rates of the new soft drugs can be
controlled by structural modifications.

6. Active metabolite based soft drug
According to Bodor it is
preferable to use as the
drug of choice an active
species which under goes
a one step singular,
predictable
metabolic deactivation.
It's refers to product of a
drug having the same
affinity as parent drug.

7. Clinical Success Stories
Rationally design soft drugs that reached
Marketing approval include,for example:
the ultra-short-acting soft calcium
channel blocker clevidipine approved
for i.v use in the reduction and control of
blood pressure in cardiac
surgical procedures.

8. Future Perspective
Soft drugs are especially likely to succeed in areas where
the desired activity is localized &relatively short-
lived.For example:in dermatology,where topical application
is convenient,as the skin is easily accesible and Localize activity is
particularly desirable.

9. CONCLUSION
Soft drug design is part of the more
general retrometabolic drug design concept.It is very
general and can be applied in a wide range of therapeutic
areas to generate innovative,new chemical entities.

10. References
Bodor N, Buchwald P. Soft drug design: general principles and recent applications. Medicinal research
reviews. 2000 Jan;20(1):58-101.
Bodor N. Designing safer drugs based on the soft drug approach. Trends in Pharmacological Sciences.
1982 Jan 1;3:53-6.
https://cleviprex.com/dosing-administration/
Bodor N, Oshiro Y, Loftsson T, Katovich M, Caldwell W. Soft Drugs VI. The Application of the Inactive
Metabolite Approach for Design of Soft β-Blockers1? 2. Pharmaceutical research. 1984 May;1(3):120-5.
https://www.colleyvilledermatology.com/dermatology-services/medical-dermatology/

11. THANK YOU