Riccardo Vergaro
@drvergaro.bsky.social
Resident in Anesthesiology, Intensive care & Pain medicine - IRCCS San Matteo, Pavia
WO2025249542 describes a first-in-class HIV ADC linking a CD4-mimetic to a broadly neutralising antibody. The dual mechanism induces gp120 misfolding and blocks entry/replication, improving potency, breadth and in-vivo durability vs prior CD4 mimetics.
[Credit: Kumamoto University]
[Credit: Kumamoto University]
December 15, 2025 at 10:28 AM
WO2025249542 describes a first-in-class HIV ADC linking a CD4-mimetic to a broadly neutralising antibody. The dual mechanism induces gp120 misfolding and blocks entry/replication, improving potency, breadth and in-vivo durability vs prior CD4 mimetics.
[Credit: Kumamoto University]
[Credit: Kumamoto University]
WO2025248500 describes ENPP3-targeting ADCs for RCC, HCC, NSCLC and hematologic cancers, using defined antibodies, Fc N297 glycan site-specific conjugation and diverse auristatin payloads with optimized cleavable linkers to improve stability, DAR control and reduce off-target toxicity.
[Credit: J&J]
[Credit: J&J]
December 14, 2025 at 2:03 PM
WO2025248500 describes ENPP3-targeting ADCs for RCC, HCC, NSCLC and hematologic cancers, using defined antibodies, Fc N297 glycan site-specific conjugation and diverse auristatin payloads with optimized cleavable linkers to improve stability, DAR control and reduce off-target toxicity.
[Credit: J&J]
[Credit: J&J]
WO2025247330 discloses bispecific EGFR×c-Met ADCs with novel antibody sequences and optimized auristatin/TOPO1 linker-payloads, improving dual-positive tumour selectivity, internalisation, DAR control, stability, and efficacy while reducing EGFR-related toxicity.
December 13, 2025 at 11:55 AM
WO2025247330 discloses bispecific EGFR×c-Met ADCs with novel antibody sequences and optimized auristatin/TOPO1 linker-payloads, improving dual-positive tumour selectivity, internalisation, DAR control, stability, and efficacy while reducing EGFR-related toxicity.
The patent describes tumour-targeted multispecific fusion proteins that bind TAAs, deliver CD28 co-stimulation, and engage CD80/CD86 to restore APC–T-cell signalling. This design aims to rebuild the immune synapse locally while avoiding systemic CD28-driven toxicity.
[Credit: Adlai Nortye]
[Credit: Adlai Nortye]
December 12, 2025 at 12:58 PM
The patent describes tumour-targeted multispecific fusion proteins that bind TAAs, deliver CD28 co-stimulation, and engage CD80/CD86 to restore APC–T-cell signalling. This design aims to rebuild the immune synapse locally while avoiding systemic CD28-driven toxicity.
[Credit: Adlai Nortye]
[Credit: Adlai Nortye]
pH-dependent anti-cMET ADCs bind strongly at neutral pH and release in acidic endosomes, enabling receptor recycling, repeated uptake, and higher payload delivery. This boosts killing of low-cMET tumours and overcomes resistance seen with prior MET- or EGFR-targeted therapies.
[Credit: Mythic Ther.]
[Credit: Mythic Ther.]
December 11, 2025 at 1:45 PM
pH-dependent anti-cMET ADCs bind strongly at neutral pH and release in acidic endosomes, enabling receptor recycling, repeated uptake, and higher payload delivery. This boosts killing of low-cMET tumours and overcomes resistance seen with prior MET- or EGFR-targeted therapies.
[Credit: Mythic Ther.]
[Credit: Mythic Ther.]
A new antibody–cytokine platform uses non-cleavable cytomasking linkers to stably suppress cytokine activity in circulation. Masking lifts only upon antigen binding, enabling localized activation, limiting off-target inflammation, and preserving full potency of IL-2/12/15/21.
[Credit: OSE Immunoth]
[Credit: OSE Immunoth]
December 10, 2025 at 9:46 AM
A new antibody–cytokine platform uses non-cleavable cytomasking linkers to stably suppress cytokine activity in circulation. Masking lifts only upon antigen binding, enabling localized activation, limiting off-target inflammation, and preserving full potency of IL-2/12/15/21.
[Credit: OSE Immunoth]
[Credit: OSE Immunoth]
Oncology dominated 2025 FDA small-molecule approvals, joined by immunology and genetic diseases. Big Pharma players like Bayer, BI, Novartis, and Sanofi won multiple approvals, while mid-sized biotech firms drove niche innovation. The landscape is diverse yet heavily focused on cancer therapeutics.
December 9, 2025 at 9:55 AM
Oncology dominated 2025 FDA small-molecule approvals, joined by immunology and genetic diseases. Big Pharma players like Bayer, BI, Novartis, and Sanofi won multiple approvals, while mid-sized biotech firms drove niche innovation. The landscape is diverse yet heavily focused on cancer therapeutics.
Anti-CDH17 ADCs target the extracellular domain of tumor-overexpressed CDH17, exploiting its limited normal-tissue expression. The patent defines high-specificity antibodies and Dxd-like ADCs to treat CDH17-positive gastric, colorectal, pancreatic, and other GI cancers.
[Credit: HZH Pharmaceutical]
[Credit: HZH Pharmaceutical]
December 8, 2025 at 8:36 AM
Anti-CDH17 ADCs target the extracellular domain of tumor-overexpressed CDH17, exploiting its limited normal-tissue expression. The patent defines high-specificity antibodies and Dxd-like ADCs to treat CDH17-positive gastric, colorectal, pancreatic, and other GI cancers.
[Credit: HZH Pharmaceutical]
[Credit: HZH Pharmaceutical]
Fusion proteins pairing high-affinity PD-1 binders with RGD or TGF-β–related peptides boost tumour targeting, ease stromal and TGF-β–driven suppression, and improve T-cell access. These modular constructs enhance localisation, dual-pathway immune activation, and overall anti-tumour efficacy.
December 7, 2025 at 3:00 PM
Fusion proteins pairing high-affinity PD-1 binders with RGD or TGF-β–related peptides boost tumour targeting, ease stromal and TGF-β–driven suppression, and improve T-cell access. These modular constructs enhance localisation, dual-pathway immune activation, and overall anti-tumour efficacy.
W02025241603 discloses a controlled method to convert maleimide thiosuccinimide linkages into fully opened, stable forms, enabling uniform bis-open-ring bis-maleimide ADCs with improved in-vivo stability, longer half-life, reduced toxicity, reproducible DAR≈4, and superior antitumor efficacy.
December 6, 2025 at 11:24 AM
W02025241603 discloses a controlled method to convert maleimide thiosuccinimide linkages into fully opened, stable forms, enabling uniform bis-open-ring bis-maleimide ADCs with improved in-vivo stability, longer half-life, reduced toxicity, reproducible DAR≈4, and superior antitumor efficacy.
Annexin A5 conjugated to multiple cytotoxic payloads targets phosphatidylserine exposed on stressed cells. This enables selective binding and drug delivery to cancer, bacterial, fungal, and parasitic cells, offering a broad, resistance-evading alternative to antigen-specific ADCs and antibiotics.
December 5, 2025 at 7:30 AM
Annexin A5 conjugated to multiple cytotoxic payloads targets phosphatidylserine exposed on stressed cells. This enables selective binding and drug delivery to cancer, bacterial, fungal, and parasitic cells, offering a broad, resistance-evading alternative to antigen-specific ADCs and antibiotics.
New maleimide-derived ADC linkers self-hydrolyze at ~pH 7, stabilizing thiosuccinimide without harsh alkaline treatment. This avoids antibody damage, prevents payload transfer to off-target thiols, improves manufacturability, and yields more stable, consistent in-vivo performance.
[Credit: BeOne]
[Credit: BeOne]
December 4, 2025 at 1:31 PM
New maleimide-derived ADC linkers self-hydrolyze at ~pH 7, stabilizing thiosuccinimide without harsh alkaline treatment. This avoids antibody damage, prevents payload transfer to off-target thiols, improves manufacturability, and yields more stable, consistent in-vivo performance.
[Credit: BeOne]
[Credit: BeOne]
New PLK1-targeted PROTACs designed as DAC payloads use dihydropteridinone or glutarimide ligands plus an E3-recruiting element and optimized linkers. They enable potent, selective PLK1 degradation, plasma-stable antibody conjugation and strong cytotoxicity after tumor-cell uptake.
[Credit: UPPTHERA]
[Credit: UPPTHERA]
December 3, 2025 at 2:11 PM
New PLK1-targeted PROTACs designed as DAC payloads use dihydropteridinone or glutarimide ligands plus an E3-recruiting element and optimized linkers. They enable potent, selective PLK1 degradation, plasma-stable antibody conjugation and strong cytotoxicity after tumor-cell uptake.
[Credit: UPPTHERA]
[Credit: UPPTHERA]
A CD3×BCMA bispecific redirects T cells to eradicate BCMA-positive plasma cells producing amyloidogenic light chains in AL amyloidosis. It offers a distinct, targeted option for relapsed/refractory disease, reducing light-chain output and limiting further organ damage.
[Credit: Regeneron]
[Credit: Regeneron]
December 2, 2025 at 1:24 PM
A CD3×BCMA bispecific redirects T cells to eradicate BCMA-positive plasma cells producing amyloidogenic light chains in AL amyloidosis. It offers a distinct, targeted option for relapsed/refractory disease, reducing light-chain output and limiting further organ damage.
[Credit: Regeneron]
[Credit: Regeneron]
Eli Lilly disclosed a patent for potent small-molecule amylin agonists, revealing 200+ compounds with sub-nanomolar activity. As peptide agonists show strong weight-loss potential, these data offer a foundation for competitors to design improved amylin-based metabolic therapies.
December 1, 2025 at 11:50 AM
Eli Lilly disclosed a patent for potent small-molecule amylin agonists, revealing 200+ compounds with sub-nanomolar activity. As peptide agonists show strong weight-loss potential, these data offer a foundation for competitors to design improved amylin-based metabolic therapies.
Trispecific antibodies targeting TIM-3, VISTA and a macrophage marker reprogram TAM-rich, immunotherapy-refractory tumours. By activating macrophage-intrinsic type-I IFN signalling, they bypass poor T-cell infiltration and overcome the limits of single-checkpoint blockade.
[Credit: KU Leuven]
[Credit: KU Leuven]
November 30, 2025 at 1:31 PM
Trispecific antibodies targeting TIM-3, VISTA and a macrophage marker reprogram TAM-rich, immunotherapy-refractory tumours. By activating macrophage-intrinsic type-I IFN signalling, they bypass poor T-cell infiltration and overcome the limits of single-checkpoint blockade.
[Credit: KU Leuven]
[Credit: KU Leuven]
FAP9 is a chemically stable ligand targeting FAP-expressing myofibroblasts in fibrotic disease. It resists acid/base/heat degradation, improving specificity and retention. FAP9-conjugates enable targeted delivery of PI3K or TGF-β inhibitors to reduce fibroblast activation and matrix buildup.
November 29, 2025 at 1:39 PM
FAP9 is a chemically stable ligand targeting FAP-expressing myofibroblasts in fibrotic disease. It resists acid/base/heat degradation, improving specificity and retention. FAP9-conjugates enable targeted delivery of PI3K or TGF-β inhibitors to reduce fibroblast activation and matrix buildup.
LaNova's new ADC targeting tumour-specific Sialyl-Tn, a truncated O-glycan overexpressed in most carcinomas. High-affinity anti-STn antibodies internalise efficiently, enabling potent payload delivery. Resulting ADCs show strong cytotoxicity, by-stander effect, and marked in-vivo tumour suppression.
November 28, 2025 at 9:29 AM
LaNova's new ADC targeting tumour-specific Sialyl-Tn, a truncated O-glycan overexpressed in most carcinomas. High-affinity anti-STn antibodies internalise efficiently, enabling potent payload delivery. Resulting ADCs show strong cytotoxicity, by-stander effect, and marked in-vivo tumour suppression.
A novel therapy pairs an IgG-degrader with a monoclonal antibody to remove IgG-based ADAs via FcRn blockade or lysosomal targeting. By clearing neutralising and non-neutralising ADAs, it restores biologic PK/PD and efficacy in autoimmune and inflammatory diseases.
[Credit: Biohaven]
[Credit: Biohaven]
November 27, 2025 at 1:26 PM
A novel therapy pairs an IgG-degrader with a monoclonal antibody to remove IgG-based ADAs via FcRn blockade or lysosomal targeting. By clearing neutralising and non-neutralising ADAs, it restores biologic PK/PD and efficacy in autoimmune and inflammatory diseases.
[Credit: Biohaven]
[Credit: Biohaven]
T-cell immunotherapy has progressed from CP blockade to engineered cells and engagers, but solid tumours remain challenging. Cytokines are central to T-cell efficacy; new Roche's tumour-targeted, safer cytokine variants aim to boost local CD8⁺ T-cell activity and strengthen combination therapies.
November 26, 2025 at 12:10 PM
T-cell immunotherapy has progressed from CP blockade to engineered cells and engagers, but solid tumours remain challenging. Cytokines are central to T-cell efficacy; new Roche's tumour-targeted, safer cytokine variants aim to boost local CD8⁺ T-cell activity and strengthen combination therapies.
Innate's anti-CD73 plus T-cell engager therapy counters adenosine-driven immunosuppression, restores T-cell activity, and boosts TCE cytotoxicity in B-cell malignancies. Preclinical DLBCL models show strong synergy, including at lower TCE doses, suggesting reduced CRS risk and improved durability.
November 25, 2025 at 11:41 AM
Innate's anti-CD73 plus T-cell engager therapy counters adenosine-driven immunosuppression, restores T-cell activity, and boosts TCE cytotoxicity in B-cell malignancies. Preclinical DLBCL models show strong synergy, including at lower TCE doses, suggesting reduced CRS risk and improved durability.
Antibody-conjugated nanoparticles deliver mRNA across the BBB by targeting luminal brain endothelial antigens, enabling transcytosis, intracellular mRNA release, and directional secretion of therapeutic proteins into the CNS. This non-viral platform offers targeted, transient, safer brain delivery.
November 24, 2025 at 1:32 PM
Antibody-conjugated nanoparticles deliver mRNA across the BBB by targeting luminal brain endothelial antigens, enabling transcytosis, intracellular mRNA release, and directional secretion of therapeutic proteins into the CNS. This non-viral platform offers targeted, transient, safer brain delivery.
Stapled scFv uses engineered disulfide bonds between VH/VL frameworks and linker cysteines to stabilize structure, limit VH/VL motion, prevent swapping and aggregation, and raise Tm, improving folding, solubility, and manufacturability without altering antigen binding.
[Credit: The Janssen Pharm]
[Credit: The Janssen Pharm]
November 23, 2025 at 1:33 PM
Stapled scFv uses engineered disulfide bonds between VH/VL frameworks and linker cysteines to stabilize structure, limit VH/VL motion, prevent swapping and aggregation, and raise Tm, improving folding, solubility, and manufacturability without altering antigen binding.
[Credit: The Janssen Pharm]
[Credit: The Janssen Pharm]
Engineered CXCL14-Fc fusion proteins improve the poor stability and short half-life of native CXCL14. By linking CXCL14 to an Fc domain, they gain prolonged exposure and enhanced activity, enabling sustained immunomodulation and tumour-suppressive effects across multiple cancers.
[Credit: Hadasit]
[Credit: Hadasit]
November 22, 2025 at 1:17 PM
Engineered CXCL14-Fc fusion proteins improve the poor stability and short half-life of native CXCL14. By linking CXCL14 to an Fc domain, they gain prolonged exposure and enhanced activity, enabling sustained immunomodulation and tumour-suppressive effects across multiple cancers.
[Credit: Hadasit]
[Credit: Hadasit]
Ig-Aim are fusion proteins linking surface-Ig–binding peptides to receptor-deficient diphtheria toxin, killing only Bcell clones with specific sIg. They spare naïve IgM⁺ cells, avoid broad B-cell depletion & enable precise removal of pathogenic IgG⁺/IgA⁺/IgE⁺ or antigen-specific clones.[Credit:IFOM]
November 21, 2025 at 10:26 AM
Ig-Aim are fusion proteins linking surface-Ig–binding peptides to receptor-deficient diphtheria toxin, killing only Bcell clones with specific sIg. They spare naïve IgM⁺ cells, avoid broad B-cell depletion & enable precise removal of pathogenic IgG⁺/IgA⁺/IgE⁺ or antigen-specific clones.[Credit:IFOM]