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Dr. NIMISHA UPADHYAY
2ND Yr PG SCHOLAR
DEPT. OF DRAVYAGUNA VIJNANA 1
CONTENTS
Introduction
Definition
Roadmap
History
Pathways
Ayurvedic approach
Scientific approach
Hurdles
Recent development
Conclusion
2
Derived from Greek words
oPharmakon - Drug
oLogos - Study
A drug is a moiety substance or chemical
entity which when consumed can intervene
at physical, physiological and
psychological levels.
3
WHAT IS PHARMACOLOGY ?
ADR
Inefficiency
of drug
Race,
Topological
area
Drug
overdose
Consumption
of drugs
water,
Alcohol or
other
narcotics
Biologic
variability
Accessibility
Cost
effectiveness
LIMITATIONS OF PHARMACOLOGY
4
• Reverse pharmacology is defined as science of
integrating documented experiments hits into leads that
are further developed into drug candidate or formulations
through more systematic and precisely designed
preclinical and clinical research.
• Salient feature of this approach is the combination of
knowledge learned from traditional or folk medicine and
the modern technology to provide better and safe leads.
REVERSE PHARMACOLOGY AND ITS APPROACH
5
A representative of a compound series with sufficient
potential to progress to a full drug development
program
Lead is derived from hit, and has the desired activity
which is confirmed upon retesting.
KEY WORDS:
A drug target is a molecule in the body, associated with a particular
disease process and that could be addressed by a drug to produce a
desired therapeutic effect.
6
7
DIFFERENTIATION
8
9
HISTORY OF REVERSE
PHARMACOLOGY IN INDIA
• Sir Gananath Sen
 Father of Reverse pharmacology
 Laid the foundation of Reverse
pharmacology of medicinal plants
In 1993
demonstrated the
antihypertensive
and tranquilizing
effect of Rawolfia
serpentina.
Also observed
unique side effect
such as depression,
extra pyramidal
syndrome and
peptic ulcers
Sir Sen
Bose and
Kartik
Bose
10
DOMAINS OF REVERSE PHARMACOLOGY
11
Experimental Hits
and Targets
Exploratory
leads
DOCKING: MOLECULAR DOCKING,PATHWAY ANALYSIS
12
RESPONSE MOLECULE
• A mechanism of action usually
includes mention of the specific
molecular targets to which the
drug binds, such as an enzyme
or receptor.
13
• Receptor sites have specific
affinities for drugs based on
the chemical structure of the
drug, as well as the specific
action that occurs there.
EVIDENCE BASED MEDICINE FOR RP
14
AYURVEDA AND REVERSE PHARMACOLOGY
ACTION AND
DRUG
KNOWN DRUGS
BEYOUND
ACTION
FOLKLORE
15
16
IDEAL AND
CHANGING
DECISION
AND
RESULT
AYURVEDA
IS
ETERNAL
TRANSLATIONAL AYURVEDA
Modified dosage forms
Blending of modern diagnosis with traditional use
HPTLC
Mass Spectrometry
High Throughput Screening (HTS)
Misleading Advertisement should not be
encouraged in the name of ayurveda.
SCIENTIFIC APPROACH
17
18
Despite a vast potential and possibilities- very few success stories
Most of the work in the field has remained in clinics of
traditional practitioners or confined to academic research
laboratories
Improper experimental documentation
Lack of proper identity and implementation of
good laboratory practices
Cultural prejudice for
Alien Science.
HURDLES
19
CUSTOMISED AND
PRECISION MEDICINE
20
21
RECENT DEVELOPMENT
22
23
The drug candidate is
an herbal beneficiated
extract of leaves of
Argemone mexicana
Under NMITLI, Lupin
Laboratories (India)
attempted development
of a single plant based
oral herbal formulations
through Reverse
Pharmacology
Novel mechanism of
action and effectively
modulates the cellar
function to psoriatic
lesion healing
improvement
Three main bottlenecks in drug development (Time, Money and Toxicity)
can easily addressed by reverse pharmacology.
It potentiates fast track drug development of newer, safer, and effective
drugs.
Normal drug developmental course “Laboratory to clinic” actually
becomes “Clinics to Laboratory” in RP.
These records are particularly valuable since effectively these medicines
have been tested for thousands years on people.
CONCLUSION
24
25
• Many countries are becoming extremely aware of their traditional knowledge.
• Global pharmaceuticals industry is looking for innovative solutions to re-activate and re-
energize discovery pipeline.
• Adds a new life in existing global economic environment.
• It will be the interest of pharmaceutical companies, researchers and ultimately the global
community to respect the tradition build on their knowledge and experiential wisdom
ADVANTAGES AND LIMITATIONS
26
REFERENCES
• Lagunin AA, Ivanov SM, Gloriozova TA, Pogodin PV, Filimonov DA, Kumar S, Goel
RK. Combined network pharmacology and virtual reverse pharmacology approaches for
identification of potential targets to treat vascular dementia. Sci Rep. 2020 Jan
14;10(1):257. doi: 10.1038/s41598-019-57199-9. PMID: 31937840; PMCID:
PMC6959222.
• Li L. Reverse Translational Pharmacology Research Is Driven by Big Data. CPT
Pharmacometrics Syst Pharmacol. 2018 Feb;7(2):63-64. doi: 10.1002/psp4.12277. Epub
2018 Feb 19. PMID: 29457706; PMCID: PMC5824108.
• Saeidnia S, Gohari AR, Manayi A. Reverse Pharmacognosy and Reverse Pharmacology;
Two Closely Related Approaches for Drug Discovery Development. Curr Pharm
Biotechnol. 2016;17(11):1016-22. doi: 10.2174/1389201017666160709200208. PMID:
27396403.
• Miranda Furtado CL, Dos Santos Luciano MC, Silva Santos RD, Furtado GP, Moraes
MO, Pessoa C. Epidrugs: targeting epigenetic marks in cancer treatment. Epigenetics.
2019 Dec;14(12):1164-1176. doi: 10.1080/15592294.2019.1640546. Epub 2019 Jul 13.
PMID: 31282279; PMCID: PMC6791710.
27
THANK YOU FOR
PATIENCE LISTENING
28

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REVERSE PHARMACOLOGY APPROACH

  • 1. Dr. NIMISHA UPADHYAY 2ND Yr PG SCHOLAR DEPT. OF DRAVYAGUNA VIJNANA 1
  • 3. Derived from Greek words oPharmakon - Drug oLogos - Study A drug is a moiety substance or chemical entity which when consumed can intervene at physical, physiological and psychological levels. 3 WHAT IS PHARMACOLOGY ?
  • 4. ADR Inefficiency of drug Race, Topological area Drug overdose Consumption of drugs water, Alcohol or other narcotics Biologic variability Accessibility Cost effectiveness LIMITATIONS OF PHARMACOLOGY 4
  • 5. • Reverse pharmacology is defined as science of integrating documented experiments hits into leads that are further developed into drug candidate or formulations through more systematic and precisely designed preclinical and clinical research. • Salient feature of this approach is the combination of knowledge learned from traditional or folk medicine and the modern technology to provide better and safe leads. REVERSE PHARMACOLOGY AND ITS APPROACH 5
  • 6. A representative of a compound series with sufficient potential to progress to a full drug development program Lead is derived from hit, and has the desired activity which is confirmed upon retesting. KEY WORDS: A drug target is a molecule in the body, associated with a particular disease process and that could be addressed by a drug to produce a desired therapeutic effect. 6
  • 7. 7
  • 9. 9
  • 10. HISTORY OF REVERSE PHARMACOLOGY IN INDIA • Sir Gananath Sen  Father of Reverse pharmacology  Laid the foundation of Reverse pharmacology of medicinal plants In 1993 demonstrated the antihypertensive and tranquilizing effect of Rawolfia serpentina. Also observed unique side effect such as depression, extra pyramidal syndrome and peptic ulcers Sir Sen Bose and Kartik Bose 10
  • 11. DOMAINS OF REVERSE PHARMACOLOGY 11 Experimental Hits and Targets Exploratory leads
  • 13. RESPONSE MOLECULE • A mechanism of action usually includes mention of the specific molecular targets to which the drug binds, such as an enzyme or receptor. 13 • Receptor sites have specific affinities for drugs based on the chemical structure of the drug, as well as the specific action that occurs there.
  • 15. AYURVEDA AND REVERSE PHARMACOLOGY ACTION AND DRUG KNOWN DRUGS BEYOUND ACTION FOLKLORE 15
  • 16. 16 IDEAL AND CHANGING DECISION AND RESULT AYURVEDA IS ETERNAL TRANSLATIONAL AYURVEDA Modified dosage forms Blending of modern diagnosis with traditional use HPTLC Mass Spectrometry High Throughput Screening (HTS) Misleading Advertisement should not be encouraged in the name of ayurveda.
  • 18. 18
  • 19. Despite a vast potential and possibilities- very few success stories Most of the work in the field has remained in clinics of traditional practitioners or confined to academic research laboratories Improper experimental documentation Lack of proper identity and implementation of good laboratory practices Cultural prejudice for Alien Science. HURDLES 19
  • 22. 22
  • 23. 23 The drug candidate is an herbal beneficiated extract of leaves of Argemone mexicana Under NMITLI, Lupin Laboratories (India) attempted development of a single plant based oral herbal formulations through Reverse Pharmacology Novel mechanism of action and effectively modulates the cellar function to psoriatic lesion healing improvement
  • 24. Three main bottlenecks in drug development (Time, Money and Toxicity) can easily addressed by reverse pharmacology. It potentiates fast track drug development of newer, safer, and effective drugs. Normal drug developmental course “Laboratory to clinic” actually becomes “Clinics to Laboratory” in RP. These records are particularly valuable since effectively these medicines have been tested for thousands years on people. CONCLUSION 24
  • 25. 25
  • 26. • Many countries are becoming extremely aware of their traditional knowledge. • Global pharmaceuticals industry is looking for innovative solutions to re-activate and re- energize discovery pipeline. • Adds a new life in existing global economic environment. • It will be the interest of pharmaceutical companies, researchers and ultimately the global community to respect the tradition build on their knowledge and experiential wisdom ADVANTAGES AND LIMITATIONS 26
  • 27. REFERENCES • Lagunin AA, Ivanov SM, Gloriozova TA, Pogodin PV, Filimonov DA, Kumar S, Goel RK. Combined network pharmacology and virtual reverse pharmacology approaches for identification of potential targets to treat vascular dementia. Sci Rep. 2020 Jan 14;10(1):257. doi: 10.1038/s41598-019-57199-9. PMID: 31937840; PMCID: PMC6959222. • Li L. Reverse Translational Pharmacology Research Is Driven by Big Data. CPT Pharmacometrics Syst Pharmacol. 2018 Feb;7(2):63-64. doi: 10.1002/psp4.12277. Epub 2018 Feb 19. PMID: 29457706; PMCID: PMC5824108. • Saeidnia S, Gohari AR, Manayi A. Reverse Pharmacognosy and Reverse Pharmacology; Two Closely Related Approaches for Drug Discovery Development. Curr Pharm Biotechnol. 2016;17(11):1016-22. doi: 10.2174/1389201017666160709200208. PMID: 27396403. • Miranda Furtado CL, Dos Santos Luciano MC, Silva Santos RD, Furtado GP, Moraes MO, Pessoa C. Epidrugs: targeting epigenetic marks in cancer treatment. Epigenetics. 2019 Dec;14(12):1164-1176. doi: 10.1080/15592294.2019.1640546. Epub 2019 Jul 13. PMID: 31282279; PMCID: PMC6791710. 27
  • 28. THANK YOU FOR PATIENCE LISTENING 28