Your Guide to Beacon ADC

Your Guide to Beacon ADC

Dataset-Specific Guide

Last Updated: 24th February 2025

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Introduction 1 Scope of Dataset Beacon ADC covers antibody drug conjugates and related therapies including immunotoxins, small molecule drug conjugates, liposomal drug conjugates, protein-drug conjugates, ligand-conjugated nanoparticles, and radioimmunoconjugates. Module launched: 2015 Diseases covered: All A conjugate consisting of a targeting moiety that is a monoclonal antibody (mAb) or a fragment thereof and a payload (or a multitude thereof) that is usually a small-molecule cytotoxic agent joined via a chemical linker. 1. ADC (Antibody-Drug Conjugate) Currently included in Beacon ADC: a. Antibody-Fragment Drug Conjugate b. Antibody-Oligonucleotide Conjugate (AOC) c. Bispecific Antibody-Drug Conjugate (Bispecific ADC) conjugate consisting of a targeting moiety that is an antibody fragment and a payload (or a multitude thereof) that is usually a small-molecule cytotoxic or non-cytotoxic agent via a chemical linker. conjugate consisting of a targeting moiety that is an antibody or a fragment thereof and a payload (or a multitude thereof) that is usually a protein degrader connected via a chemical linker. conjugate consisting of a targeting moiety that is a bispecific antibody or a fragment thereof and a payload (or a multitude thereof), typically a cytotoxic agent, connected via a chemical linker. 2 Folic acid and folate derivatives – bind to folate receptors (a protein overexpressed in ovarian cancer for example) – e.g., Vintafolide Glutamic acid urea derivatives – bind to prostate-specific membrane antigen (a surface marker of prostate cancer cells) A conjugate consisting of a targeting moiety that is a small organic ligand or a synthetic peptide (<100 a.a.)="a.a.)" chemically="chemically" linked="linked" to="to" a="A" payload="payload" (or="(or" multitude="multitude" thereof)="thereof)" that="that" is="is" usually="usually" small-molecule="small-molecule" cytotoxic="cytotoxic" agent.="agent." examples="Examples" of="of" small="Small" organic="organic" ligands="ligands" 3.="3." molecule="Molecule" drug="Drug" conjugates="Conjugates" fusion="fusion" protein="protein" consisting="consisting" targeting="targeting" moiety="moiety" mab="mAb" or="or" fragment="fragment" thereof="thereof" and="and" biologically="biologically" active="active" thereof.="thereof." the="The" typically="typically" (derived="(derived" from)="from)" microorganism="microorganism" plant.="plant." 2.="2." immunotoxin="Immunotoxin" d.="d." degrader-antibody="Degrader-Antibody" conjugate="conjugate" (dac)="(DAC)" e.="e." dual-payload="Dual-Payload" antibody-drug="Antibody-Drug" (dual-payload="(Dual-Payload" adc)="ADC)" an="an" antibody="antibody" degrader="degrader" connected="connected" via="via" chemical="chemical" linker.="linker." two="two" distinct="distinct" payloads,="payloads," agents="agents" modulatory="modulatory" compounds,="compounds," linkers.="linkers." synthetic="synthetic" peptide="peptide" (="("><100 3="3" a.a.)="a.a.)" chemically="chemically" linked="linked" to="to" a="A" payload="payload" (or="(or" multitude="multitude" thereof)="thereof)" that="that" is="is" usually="usually" small-molecule="small-molecule" cytotoxic="cytotoxic" or="or" non-cytotoxic="non-cytotoxic" agent.="agent." 4.="4." peptide="peptide" drug="Drug" conjugate="conjugate" 5.="5." protein="Protein" 6.="6." antibody-conjugated="Antibody-Conjugated" nanoparticle="nanoparticle" 7.="7." radioconjugate="Radioconjugate" 8.="8." radioimmunoconjugate="Radioimmunoconjugate" 9.="9." ligand-conjugated="Ligand-conjugated" 10.="10." antibody-liposomal="Antibody-Liposomal" consisting="consisting" of="of" targeting="targeting" molecule="molecule" recombinant="recombinant" (="(">100 a.a.) or protein molecule but NOT a mAb or a fragment thereof and a payload (or a multitude thereof) that is usually a small-molecule cytotoxic agent via a chemical linker. E.g., Affimer A conjugate consisting of a targeting moiety that is small molecules or other modalities and a payload (or a multitude thereof) that is a radioactive or radiolabelled molecule via a chemical linker. A conjugate of a nanoparticle chemically conjugated to targeting moieties that are antibodies or fragments thereof to deliver the payload. A conjugate consisting of a targeting moiety that is a monoclonal antibody (mAb) or a fragment thereof and a payload (or a multitude thereof) that is a radioactive or radiolabelled molecule via a chemical linker. A conjugate of a nanoparticle chemically conjugated to targeting moieties that are small molecules or other modalities to deliver the payload. A conjugate of a liposome chemically conjugated to targeting moieties that are antibodies or fragments thereof to deliver the payload. 4 Not currently included in Beacon ADC: Radioconjugates which are imaging agents. 5 Use Case 1 Understand how to use filters for a drugs search - Payload. We will use an example case of searching for all classical ADC drugs with Payload MMAE being studied for the treatment of Breast Cancer. 21 2 From the Datasets, select ADC. On the Explore Data tab, select Drugs. Note: You can only select dataset(s) you are subscribed to. To broaden your search to other datasets, please email [e-mail] or contact your account manager for more information. 1 21 In Disease Indication, start typing Breast Cancer and select it from the dropdown. In Therapeutic Class, start typing ADC/Antibody drug conjugates and select it from the dropdown. 6 4 3 In Payload, start typing MMAE and select it from the dropdown. 5 21 7 6 Click Search to load your results. Note: To learn more about managing columns or navigating through drug records please check the guides: Managing search results and Navigating a Drug Page. 21 Use Case 2 8 2 From the Datasets, select ADC. On the Explore Data tab, select Trials. Note: You can only select dataset(s) you are subscribed to. To broaden your search to other datasets, please email [e-mail] or contact your account manager for more information. 1 Understand how to use filters for a trials search - Targets and Combination. We will use an example use case to find all TROP-2 targeting ADC trials being studied in combination with an Immune Checkpoint Modulator. 21 Click + Add New Combination to search for combination trials. 9 In Drug Targets, start typing TROP-2 and select it from the dropdown. 5 3 4 Add further Advanced Filters that you would like to view. 10 Click on Search in Arms to load the results where the drug combinations exist within one or more arms of the trial and then click on Search button to load your results. 6 Note: To learn more about managing columns or navigating through trial records please check the guides: Managing search results and Navigating a Trial Page. 5 In the Combination search filters, start typing Immune Checkpoint Modulator in Therapeutic Class and select it from the dropdown. 11 Glossary Conjugation Amino Acid: The amino acid of the targeting moiety (protein) to where the linker-payload is attached. Conjugation site: The location in the targeting moiety (protein) where linker-payload is attached. Conjugation Technology: The technology used to conjugate a linker and payload to a targeting moiety. Drug-Antibody Ratio (DAR): The average number of drugs per targeting moiety. Drug Target: Refers to the molecule to which the drug will bind. Linker: The chemical component connecting the targeting moiety and the payload. Linker Catabolism: The methodology of releasing the payload from the targeting moiety. Payload: Any functional molecule (drug) that is attached to a targeting moiety. This may be a cytotoxic or non-cytotoxic agent. Payload Mechanism: The process describing how a drug binds to and functions at the target(s) site. Sequence and mutation: Indicates (Y/N) whether the drug record contains the sequence of the antibody, or antibody fragments that comprise the drug. Site Specifically Conjugated: Reflects if a linker-payload is attached to a targeting moiety with full positional control or stochastically. 12 Glossary Structure: The chemical structure of the targeting moiety, linker or payload. Target Binding Affinity: The binding potency of the drug for a specific target; data may include (if available) the numerical value of affinity, assay system, and cell line used. Targeting Moiety (paratope): The chemical structure- a small molecule, a peptide, or a protein (including any type of antibody), an aptamer, etc. that binds to the site of interest (epitope) within the target. Thank you for reading the Dataset-Specific Guide on ADC. If you require further support please contact us at [e-mail].</100></100>