ERIBULIN* ANTIBODY-DRUG CONJUGATE (ADC) PAYLOAD


ERIBULIN*

ERIBULIN*

Eribulin* is a fully synthetic, structurally simplified, macrocyclic ketone analogue of the marine natural product halichondrin B, produced from the marine sponge Halichondria okadai. Eribulin’s anti-tumor activity is mediated by the inhibition of microtubule elongation and mitotic spindle formation, which results in apoptosis. Eribulin mesylate, marketed as Halaven®, is an approved monotherapy in the U.S. for the treatment of metastatic breast cancer patients who previously received at least two chemotherapeutic regimens for metastatic disease. Prior therapy should have included an anthracycline and a taxane in either the adjuvant or metastatic setting.


<span>ANTI-TUMOR EFFECTS</span>

ANTI-TUMOR EFFECTS

Eribulin-based ADCs have durable anti-tumor effects in PDX models


<span>TRIPLE NEGATIVE BREAST CANCER</span>

TRIPLE NEGATIVE BREAST CANCER

Triple-negative Breast Cancer

BYSTANDER EFFECTS OF ERIBULIN ADC PAYLOAD DEMONSTRATED IN PRECLINICAL MODELS**

ERIBULIN RELEASED VIA ENDOSOMAL PROCESSING OF THE ADC DISPLAYS SUBNANOMOLAR MITOTIC AND NON-MITOTIC EFFECTS ON BOTH THE TUMOR AND TUMOR MICROENVIRONMENT

  • The mitotic effects eribulin exhibited as a payload not only include direct cytotoxic effects on receptor-positive cells bound by the ADC, but also on neighboring receptor-negative tumor cells.
  • This bystander effect on neighboring receptor-negative tumor cells showed synergistic reduction in growth of heterogeneous patient-derived xenograft (PDX) tumors.
  • Furthermore, released eribulin is highly cytotoxic to the stromal cancer-associated fibroblasts that are critical to supporting tumor growth in many cancers. 

ERIBULIN ALSO HAS COMPLEX NON-MITOTIC EFFECTS ON THE TUMOR MICROENVIRONMENT

  • Eribulin induces vascular remodeling and increases blood perfusion in tumors, thus making a greater percentage of the tumor susceptible and sensitive to subsequently administered therapies.
  • Eribulin promotes a mesenchymal-to-epithelial transition (MET) phenotype in tumors, leading to reduced metasticity, reduced immunosuppression and increased drug sensitivity.

LICENSING OPPORTUNITIES

To learn more about eribulin as an ADC payload and licensing opportunities, please call 1-877-327-5388 to speak with a member of our Business Development team.