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Chemistry Information Necessary to Support an IND

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Chemistry Information Necessary to Support an IND Application William C. Timmer, Ph.D. U.S. Food & Drug Administration Center for Drug Evaluation & Research (CDER) Office of New Drug Chemistry 301-827-1522 timmerw@cder.fda.gov

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Chemistry Information Necessary to Support an IND Application : Chemistry Information Necessary to Support an IND Application William C. Timmer, Ph.D. U.S. Food & Drug Administration Center for Drug Evaluation & Research (CDER) Office of New Drug Chemistry 301-827-1522 timmerw@cder.fda.gov

Food & Drug Administration : Food & Drug Administration

Regulatory Submissions* : Regulatory Submissions* IND: Investigational New Drug application: application to begin testing of a new drug in humans NDA: New Drug Application application to market a new drug in humans *CDER; CBER: INDs & BLAs

IND Clinical Development Phases : IND Clinical Development Phases Phase I: Safety study; first use of drug in humans; 20 - 50 healthy patients.  70% of drugs pass Phase II: Dose-ranging study; msmt of effectiveness; continued safety studies. 100s of patients.  33% of drugs pass Phase III: Efficacy study; pivotal clinical trials; 1000s of patients.  25% of drugs pass file NDA

IND / NDA Review Team : IND / NDA Review Team Recommendation Clinical Chemistry Statistics BioPharm Pharm/Tox IND NDA

Drug Approval Criteria : Drug Approval Criteria

Two Criteria for NDA Approval : Two Criteria for NDA Approval #1. Drug is safe. #2. Drug is efficacious. (mechanism of action: no!)  Simplicity of slide does not imply simple to do.

Drug Development Timeline : Drug Development Timeline PRE-CLINICAL RESEARCH CLINICAL STUDIES NDA REVIEW POST MARKETING DISCOVERY/SCREENING SYNTHESIS AND PURIFICATION ANIMAL TESTING PHASE III ADVERSE REACTION SURVEILLANCE PRODUCT DEFECT REPORTING SURVEYS SAMPLING TESTING POST APPROVAL INSPECTIONS AVG: 18 MOS. AVG: 5 YEARS AVG: 12 MOS. PHASE II PHASE I

Slide9 : CHEMISTRY (CMC) Chemistry, Manufacturing, and Controls

Office of New Drug Chemistry (ONDC) : Office of New Drug Chemistry (ONDC) To ascertain the: identity, strength, quality & purity of the new drug product  includes evaluation of manufacturing process  stability program

ONDC Staff Profile : ONDC Staff Profile Scientific Staff: ~ 30 Managers and Team Leaders ~ 100 Primary Reviewers Background: organic, analytical, physical, medicinal and pharmaceutical chemistry, biology, microbiology, biochemistry and pharmacy Education: Ph.D., M.S., B.S., B. Pharm.

Slide12 : CMC Regulatory Requirements

What’s Important from a Chemistry Perspective? : What’s Important from a Chemistry Perspective? drug substance (DS) can be quantitatively assayed in the drug product (DP). (drug product = drug substance + excipients) impurity profile of the DS: be determined be determined in the DP be qualified by Pharm/Tox reviewer

What’s Important from a Chemistry Perspective ? : What’s Important from a Chemistry Perspective ? stability of the DP be determined i.e., the physico-chemical properties of the DP have not changed over shelf-life period / clinical trial analytical test procedures and acceptance criteria are indicative of product quality batch-to-batch variations are minimized by compliance with cGMP

What is cGMP? : What is cGMP? regulations that govern: manufacturing, testing, processing, record keeping, packing, etc. rationale: assure drug product quality inspection of manufacturing site performed by trained ORA inspector (new initiative: include reviewers) compliance with cGMP regulations is required for approval of NDA GMP becomes more important as drug move to NDA. GMP is important to address early. (quality is built in)

What is the Minimum CMC Data Set? : What is the Minimum CMC Data Set? Need assay (generally HPLC) to determine: purity of DS purity of DS in DP impurities Stability data: sufficient to cover clinical trial (phase I) Labeling (Caution statement ….)

Slide17 : OTHER USEFUL REFERENCES

FDA Guidance Documents : FDA Guidance Documents www.fda.gov/cder/guidance/index.htm Guideline for the Format and Content of the CMC Section of an Application; INDs for Phase 2 and 3 Studies: CMC Information Background: FD&C Act of 1938: “The Act” 21 CFR “The Regulations” Guidance Documents

FDA Reference: ICH : FDA Reference: ICH ICH: International Conference on Harmonization www.ich.org ICH topics divided into four major categories: Q Quality Topics: relating to chemical & pharmaceutical Quality Assurance. Ex: Q1 Stability Testing, Q3 Impurity Testing These are how to do it manuals.

FDA Reference: ICH : FDA Reference: ICH S Safety Topics: relating to in vitro & in vivo pre- clinical studies. Ex: S1 Carcinogenicity Testing, S2 Genotoxicity Testing E Efficacy: relating to clinical studies in humans subject. M Multidisciplinary Topics: cross-cutting topics which do not fit into one of the above. ICH is for NDA! (but ….)

Literature Reference : Literature Reference

Literature Reference : Literature Reference Drug Information J. 37, 407-38 (2003)

Slide23 : from: Drug Information J. 37, 407-38 (2003)

Slide24 : from: Drug Information J. 37, 407-38 (2003)

Slide25 : Professional Organizations 1. DIA: Drug Information Association www.diahome.org 2. PERI: Pharmaceutical Education and Research Institute www.peri.org 3. RAPS: Regulatory Affairs Professional Society www.raps.org 4. Regulatory sections within your drug’s professional association. Organizations

Where to Go for More Information : Where to Go for More Information FDA !! Simple Two Step Process: Step 1: Prepare briefing package outlining plans/questions Step 2: Request pre-IND meeting from appropriate FDA division.

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