APL-106: (uproleselan): E-Selectin
APL-106, or Uproleselan (yoo’ pro le’ sel an), is a specific E-Selectin antagonist. In many hematologic cancers, E-Selectin plays a critical role in binding cancer cells within vascular niches in the bone marrow, which prevents the cells from entering the circulation where they can be more readily killed by chemotherapy. As supported by studies in animal models, we consider that APL-106 has the potential to improve chemotherapy response rates, duration of remission and, ultimately, survival in patients with hematologic cancers such as AML.
E-Selectin, also known as CD62E, is an adhesion receptor expressed by endothelial cells in blood vessels and vascular niches of bone marrow. It is a transmembrane glycoprotein belonging to the selectin protein family. Selectins are involved in inflammation, immunity and hemostasis, as well as cancer metastasis under cancer disease conditions. In cancer disease conditions, E-Selectin is involved in initiating adhesion event during metastasis. It binds to cancer cells through carbohydrate ligands, the enhanced expression of which is frequently associated with cancer progression and poor prognosis. E-Selectin binding to cancer cells enhances their adhesion to endothelium, including in bone marrow niches, thereby preventing them from entering circulation and shielding them from chemotherapy. It also alters the gene expression and activate survival pathways of cancer cells.
Uproleslean has received the following regulatory designations:
- NMPA Breakthrough Therapy Designation for the treatment of patients with relapsed/refractory AML
- FDA Breakthrough Therapy Designation for the treatment of adult patients with relapsed/refractory AML
- FDA Fast Track Designation for the treatment of adult patients with relapsed/refractory AML and elderly patients aged 60 years or older with AML
- FDA and EMA Orphan Drug Designation for the treatment of patients with AML
Apollomics has development and commercialization rights for APL-106 in mainland China, Hong Kong, Macau and Taiwan.
Improving sensitivity to chemotherapy in multiple hematologic cancers
- Shown preclinically to mobilize AML cancer cells out of the bone marrow
- Improved antitumor activity in combination with chemotherapy in preclinical studies
- The potential to improve chemotherapy response rates, duration of remission and, ultimately, survival in patients with hematologic cancers such as AML
Protecting against toxicities of chemotherapy
Favorable clinical safety and efficacy profiles
U.S. Partner Clinical Trials
Uproleselan was discovered and developed by GlycoMimetics, Inc., and is currently in a comprehensive Phase 3 development program in AML.