Proees, ——Duvg_Develiom | CLINICAL RESEARCH | | | Dug Dineoveyy sad _Develeprent = 1 new crags Aboug hs “thet; allow —rescarchyg — |___‘ypieatty _._seiearchers dixeover |? New insights tato__2 disease frocess— bk rp “a product_to Hep NE ‘the elects of i tar Compound te fide ben i > crt Jests_ch molecular _Confpownd _| i i a 12 Atte tay desing panty * fmayp_vumber of Concbounds look drug development disease: eee er: 4 tor er _£ = nga } > Dna di mncesstuclud es _idlertification drag Candidate, Syuthssi characterization Secening and _acsauye for therapeutic Spicy rk takes almost (a-t5yrs develop _o Single ew? ae _moleeute Bom the time _it_ is distovered then itis avaiable in marketiew for seating pecticwts. [— [spa Discover Development Process | — |) Different —tlag, which are required, o_get _spproval | dag _fay_market—ourthoria ation from food ond Dug 1 Administration. | O “Target Tenuate —___ = | ange Vebitabine _— |B tes enccin —_—____ _ | Ota pphinieaim a ———————i wpa <§_ doug din wey [Eany Drug Discovery men ) vu ; Targed derbi beaten tig Discovery Assay devel opment _ 4 Pivcoweny (it to Vea t lect Optimization Ty Visto jTn Vivo 4-_€¥-vivg Sr ADME a Pro} of, Contefr Formulation eam 2 ¢ *MleatiOn + Li. araitaty ty jms Dev i a Sama [OAT ANDA | BtAAppticatigs —— {bag Abpea [ten tice ca Drug Regicration as FDA Review : FDA Adverse Eveut Reporting System aaa oy ys lp CPAees) v | post Harkehing Monitorin i i Ci) Target Identification ~ aes By inlerachion vith targets potential drag -is assessed. sua lead Compounds are further Sereened after -asegsment ancl heer sae develop safe Serened tye ctheiy _pwopertiea aud activities cho levele p and Gcohve mediaine, i rigin of a disease _ a Tdeutijication of the Biological wigee— ah and the fotentiat targets fer ntervention cl |ye Function ‘Tsolating the agent: ( gene] muctete aed [pote in the disease oh 2 possible therapeutic & is role | bv __Characterigation of “the by the target molecular mechanisms addressed [> Aplroaches includ | + Sieg fet att | + Genetic Approaches (fenetic Polymerbhism + Connection Z the dacasc) [ changes in _mRNA| protein Aewele. (Expression profite) Phowtypie Analysis mechanisi tic Shdies b | [_* funehonal Sereening Pathway and = Invitwo cell-based, | = knotkelown , Knockout or using target Specifi'e | | PA good target should be efReacious Safe 5 stools. f+ Disease aesodahon Caenetice + expression changes) meet clinical anc Gmamnercial requirements {> Analgsic ob Sig nalig and be druggable. Pathioay ¢ Fy Rimctional Analysis Coyeresfresston—— C2) Tay get_Vatidation - sieeant Fnbeense RMA; > Torget Validation is the procec gue vavanb) dlemonety ating —the — of Functional sole the _ifentified _taeget tn | }—Ahe—dlutase _Yhenotte, = | > Target Vobdobon shows thot a molecutar target ic _divectty modulation of the inplved in a divcace — brates reetagee_% thely ty have 0. _shorateutc jet [>the teeth bara Gea fer target Vitalin a te _Uike nautt}- Validation Alproach. |. Genetic manipulation ols target genes (teboduction rs Vaslaton b | 3 ue a Gang) - Bit = knoek ing dian the gene (hewn. short Nalrbin ; Sikwa - Shork inter a MIRNA ler micro Chih the exp © aigel gene effectively a Silenced J). = cat the CRISPR- Clustered Re julety Trterspacel = short palindromic Repeats) > Genes vhich protect bacteria from adenophage. = Knocking in the gene CVirat transfection oh mutant ans) | | knock_ih knpek out i | [ine knock 1 the process ok | Chene Bhvebout ig the proses | Of Geating transgenic organitos | by Complete removal 1%; a gene, : |_Geating transgenic _organtimns by inserting a gene | A transgenic organism 2th ak _Aransgeni anew Character = nkewaeting ty the - target _with high i e-| Sumer nterathions. aa — —+ eg ates Bei |e Anbbedig: x cuk, pinged + ssnsdelecbalintel A e aud, blocked ——|J« |«chemical \_genomles ing _= chemitat_ approaches again gyre treading, proesin. it _| a Main fers the net bite Son | appty, the _tost_ identify Val Vayualia bik Series att the. —Lesk Chance of beni, | inty drug. = like Como > the Hit Finding Sales = = Kigard or weleade [fy tenis “it “sight be thse euslngenoe, — Sf or _ualerale taken Bom “the published Literature ov patents. 2) Random Serten = Usually 4 High Hroughbut Screen CTs) ye Janae _Gubound Collection (Using Commertiat| ch 3) $000 ( Stucture-baced drug design) - Tn Silico Sereenig i Compound _ Glteckions including the use fy the targef protuin i 30 structure to facilitated hit finding. based on protein ie Structure or thou Mears, U) Directed Screen - Sercenraa ok Sinaller fet Ey Conta A ax Selected bared on _frios ledge oy tha tenet = 4 es Chemical class 5) Fragment _fereen - Typlestiy brandish a Peay _-Hovsand — —Slerprands_ov lest of tous molerutay Lseights (éaoo ne), Servs! ot high Concentration | 6) DNA Encoded Ubrang — ok Smabt M. an Ay anette using e _ kechwolagy — ||_20Mz | i | involves the Corjagahion of molecule toe DNA 4, othe Mit Confirmation Phase ts follouss : Wits with potential a ‘reackiul by 4 fssa4 inlerPerence |, eetusion —%% or aggregation. A actit — «Re lasting « Compouncls that weve Fou idgaet al ceerlaf target —ore__re-tested using the Same assay) Grdihony used cathe cHTSis dene cee Dase_meshanse Cuvee generation An 1050 coud or €C5D Value << salad siecle Te ge i «Check for ‘Trreversibl binding (tS ahaganel testing 1 Contismed Ith are assayed dunve wg different assay which 6 _ usually closer to tha Laget isictogi cal. bien = of si different teehndogy | Secondant Sereening. + Confirmed Wit are tested in a Raachinal T 0 asa wit | aukagowit) Or in 4 Ano. seq (agp | avtagonst) in Celtutor environ 1 Wit canbong and Clue tenng 1 frebrmireny SAR ce z *_chewial dacability + Heaicinal chemists will evaluate Compounds ity aud Flexibility trsards chemical dtwersif cation or _Ubvary _Suymthesit. —____ L(2) Lead TdentiGication = i __ |e ea ‘He process thereby. “its” From _Seveeniang ave _hansfowwed ' into” Leads." Acteding to their Synthesis Feast | a mumber oh hit dusters __ best. —?- The Key _obyective is 40 _rapidl in order ty __ienbify 2 or 3 hit Series that have. the ike de3 this process Harts by —Gnftaming that a tre Suche 4g sidiy ber of bit - Serres : within number _2| fessor tea |__whabbnchip CsAR) ¢xtsts within 2 biological fargets ok In-w. Ty__Addétion, an arly asic ment ts made of, rags foaperties to help Select__the most: Promising leads fy “> optim isa bon. A Chemical lead 1% defined as Synthetieal ly Stable, Pea aud drug tike’ moltmle active iu _pimary and Seconda, A850 ys with acceptable Specifeuity » abfintty, aud Selectivity fy Aanget veceptor WH je abo Calleel au developmental Condidet, Charocterstic, of a Chemical Jéacl ane + * SAR dapined 6 Drig Ability | Chrebintnara jpolu'ty HERG — Codes for Kvit-l Chrokin) e 0 Vv fhe alpha Subunit of kt ion chaned) Synthetic fea: bite Select mMechanis be. assays Tn Vibro “assessment ok deus, Resistance and efftax poten bal S Evidence tn vivo Pk| Toletty of chemical lacs known based on petiminang nxieite or_in Silico Studies Cused to generate new! Wit Series with — improved properties) oe Desg} —Abity sessment _it_inborant in tpainfamisg © Gnpouod — v fom «lead molecule nto a drug. other “Assays will ereluate the potendial foaiety the Gust in, Sereens | Such as tha Ames test eurcl - Gitytoyisty Assay ¢ 4High throug but DuPK (drug metabotivon and pharmnacobaneti —|__ have become om essential ful _of Jina pti satin Haut cl) lead Optimisation saint Ang Above trl. Bom hil tea nign engi Senn 184th, fo atest jpomising_Gompouds oy the _ohjective th lead optimisation Ge is f2 _ddiver_one or dinical candidate for evaluation ino formal. regulatory CtatP) mort rior 40 human dlinteal dials. programme Lend_optimization isthe. _pouss by which & drug candidate _ ix__daigned —_after_ on tribal Jena Gorpound is idewbified, 5 fotentiat Leads _ave_ evaluated Soy a range of properties , including aud Gindiug _raechonims during, lead optimization, 3s the Ft step ing Sage dang Aeogey \s “the pinpose blend optinizstion ib fo mainbaon favre _ lead _Gmpounds , while ivproving on deficiencies in 2 _|___fraperties in | dead —_shuclure. : 3 Tn _ordey +o poduce © pre-clinical Ansa Crudidate , “He chemical Shuachures oh, eed _Constouncls Unall molto) nee to be altered | 40 _tuprove tuagest Sheu huthy aud Scleehw'ty.. 7 |» Pharmatokinekity dnd pharinntodynomit ferameters and _trxieclogial |__hofetin are oho _eveluated. 7 1) Sevens the tudertteuatng aud predict +} ty_VWivo Ipharmaesleinestts wing invite tests. 9 In order Ae MAKE daagy with higher potency and SeepJoofiles , chemreal modiftatune _do__sthe Shnrthuve “htt aug are _macle —_ dhrounh ophinv dahon . > MALDE imaging is_'4 key «-technidve for evaluating diy Canditlares anc _“their_ metabolites _in issue steuchwe rabidyy ~ Additionally, WMP fagmsuit — boned | Seraning CFS) in thy pharmaceutical lrnlusibg: hoy become toidela applred Nedle| — for the discovers aid optimization Of) bead molecule in targeted Seren Cambaizins. lintel Shady aid Resterch - shicky aes | Velden that 3 fettended sober oe aa adel to medieat as & Howley. 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