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Bioconjugates: Combining the Best of Biologics and Small Molecules

Bioconjugates are molecules formed by chemically linking two or more molecules, typically involving a biological molecule like a protein, enzyme, or antibody, with another entity, often a therapeutic agent or a diagnostic marker. They are widely used in drug development, diagnostics, and therapeutic applications due to their ability to enhance the specificity and efficacy of treatments.

Bioconjugates: Combining the Best of Biologics and Small Molecules

Key Components of Bioconjugates:

  • Biological molecule: Usually proteins, peptides, antibodies, or nucleic acids that target specific cells or biological pathways.

  • Therapeutic agent: This could be a small molecule drug, radioisotope, toxin, or other active agents.

  • Linker: The chemical entity that connects the biological molecule with the therapeutic agent, which can influence the stability, release mechanism, and overall efficacy of the bioconjugate.

Applications of Bioconjugates:

  • Antibody-Drug Conjugates (ADCs): Combining monoclonal antibodies with potent cytotoxic drugs for targeted cancer therapies. The antibody targets specific cancer cells, while the drug works to destroy them.

  • Targeted Drug Delivery: Bioconjugates help in delivering drugs specifically to diseased cells, minimizing the impact on healthy cells.

  • Diagnostics: Used in creating targeted imaging agents for more accurate diagnostic techniques, such as attaching a fluorescent molecule to an antibody for cancer detection.

  • Vaccines: Conjugate vaccines, where antigens are linked to carrier proteins to enhance immune response.

Bioconjugates Market Size Estimates

Global Bioconjugates Market: Estimated at approximately USD 5.7 billion. Antibody-drug conjugates (ADCs) account for the largest share of this market due to their success in oncology treatments.

Projected Growth: The market is expected to grow at a compound annual growth rate (CAGR) of 15-20% over the next 5-7 years. By 2030, the bioconjugates market is expected to reach USD 15-20 billion.

Global Regulation of Bioconjugates

The USFDA (U.S. Food and Drug Administration) and the EMA (European Medicines Agency) have developed regulatory frameworks to ensure the safety, efficacy, and quality of bioconjugates, particularly antibody-drug conjugates (ADCs) and other targeted biologics.

FDA Regulations on Bioconjugates

The FDA regulates bioconjugates primarily through the Center for Drug Evaluation and Research (CDER) andCenter for Biologics Evaluation and Research (CBER) depending on the nature of the product. Since bioconjugates are often considered biological products, they are regulated under the Biologics License Application (BLA) pathway, particularly when they involve large biological molecules like antibodies.

EMA Regulations on Bioconjugates

In Europe, bioconjugates are regulated by the EMA through its Committee for Medicinal Products for Human Use (CHMP). The regulatory framework is similar to the FDA, focusing on safety, efficacy, and quality.

Key industry players in the bioconjugates field and their pipeline

Seagen (formerly Seattle Genetics)

Key Products: Adcetris (brentuximab vedotin), Padcev (enfortumab vedotin).

Pipeline:

  • Tisotumab vedotin: ADC for cervical cancer (in partnership with Genmab).

  • Disitamab vedotin: ADC targeting HER2-positive cancers, including breast and gastric cancers.

  • SGN-CD228A: ADC targeting CD228 for solid tumors, in early-stage trials.

  • Ladiratuzumab vedotin: ADC for triple-negative breast cancer.

Roche/Genentech

Key Products: Kadcyla (ado-trastuzumab emtansine), Polivy (polatuzumab vedotin).

Pipeline:

  • Trastuzumab duocarmazine (SYD985): ADC targeting HER2-positive breast cancer (in collaboration with Byondis).

  • Glofitamab: A bispecific antibody that acts similarly to bioconjugates for B-cell lymphoma.

  • RG6264 (Anti-Trop2 ADC): ADC for solid tumors in Phase 1 clinical trials.

Pfizer

Key Products: Besponsa (inotuzumab ozogamicin).

Pipeline:

  • PF-06647020: ADC targeting PTK7 in solid tumors, including ovarian and breast cancer.

  • PF-06804103: ADC targeting HER2-positive cancers, including breast cancer.

  • PF-06821497: Small molecule targeting hematologic malignancies, though not a classic bioconjugate, it's a part of their targeted delivery technologies.

AstraZeneca

Key Products: Enhertu (fam-trastuzumab deruxtecan-nxki) in collaboration with Daiichi Sankyo.

Pipeline:

  • DS-1062a (Datopotamab deruxtecan): ADC targeting TROP2 for non-small cell lung cancer (NSCLC) and other solid tumors.

  • MEDI2228: ADC targeting BCMA for multiple myeloma.

  • AZD8205: ADC in early clinical stages for HER2-expressing cancers.

Daiichi Sankyo

Key Products: Enhertu (fam-trastuzumab deruxtecan), co-developed with AstraZeneca.

Pipeline:

  • DS-1062a (Datopotamab deruxtecan): Targeting TROP2 for lung cancer and breast cancer.

  • DS-7300a: ADC targeting B7-H3 for solid tumors, currently in clinical trials.

  • U3-1402: ADC targeting HER3 for lung cancer and other HER3-expressing cancers.

AbbVie

Key Products: Previously developed Rova-T (rovalpituzumab tesirine) for small-cell lung cancer, though this program was discontinued.

Pipeline:

  • ABBV-011: ADC targeting DLL3 for small-cell lung cancer.

  • ABBV-085: ADC targeting LRRC15 for sarcomas and other cancers, in Phase 1.

  • ABBV-3373: ADC for rheumatoid arthritis, combining anti-TNF with a glucocorticoid receptor modulator.

Merck

Key Products: Collaborations with ADC Therapeutics and ImmunoGen.

Pipeline:

  • XMT-2056: A novel ADC targeting HER2, co-developed with Mersana Therapeutics.

  • VLS-101: ADC targeting ROR1 for treating hematologic malignancies (in collaboration with VelosBio).

  • Lerapolturev (V937): An oncolytic virus with potential bioconjugation applications in the oncology space.

Takeda

Key Products: Adcetris (brentuximab vedotin) in collaboration with Seagen.

Pipeline:

  • TAK-500: A new ADC in clinical trials for hematologic cancers.

  • TAK-919: Focused on creating novel delivery systems combining bioconjugates with their immunology and oncology pipeline.

  • TAK-573: Investigating novel bioconjugates targeting B-cell malignancies.

Amgen

Key Products: Xgeva (denosumab) for cancer-related bone conditions.

Pipeline:

  • AMG 596: A bispecific T-cell engager (BiTE), which is a form of bioconjugate, for glioblastoma.

  • AMG 160: BiTE targeting prostate-specific membrane antigen (PSMA) in prostate cancer.

  • AMG 509: Another BiTE in development for treating prostate cancer.

ImmunoGen

Key Products: Elahere (mirvetuximab soravtansine).

Pipeline:

  • IMGN632: ADC targeting CD123 for acute myeloid leukemia (AML), in Phase 2 trials.

  • IMGN151: Next-generation ADC for ovarian and endometrial cancer, in early development.

  • IMGN779: ADC targeting CD33 for hematologic malignancies.

ADC Therapeutics

Key Products: Zynlonta (loncastuximab tesirine) for B-cell lymphoma.

Pipeline:

  • ADCT-602: ADC targeting CD22 for acute lymphoblastic leukemia (ALL).

  • ADCT-901: ADC targeting KAAG1 for solid tumors, currently in early clinical trials.

  • ADCT-701: Novel ADCs for various solid tumors, particularly in preclinical studies.

Bioconjugates, particularly antibody-drug conjugates (ADCs), are transforming the landscape of targeted therapies by offering precision in drug delivery, minimizing side effects, and improving therapeutic efficacy. Their greatest success has been in oncology, where they provide a powerful tool for delivering cytotoxic agents directly to cancer cells. As the technology matures, bioconjugates are also being explored for use in immunology, infectious diseases, and diagnostics.

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