PHARMACEUTICAL COMPOSITION FOR TREATMENT OF CANCER, COMPRISING IMMUNE CHECKPOINT INHIBITOR AND FUSION PROTEIN INCLUDING IL-2 PROTEIN AND CD80 PROTEIN

• Main Authors: NAM, Su Youn, KOH, Young Jun, KIM, Myung Hee, CHO, Young-Gyu, JANG, Myung Ho, HA, Dan Bee
• Format: Patent
• Language: English; French; Korean
• Published: 03.06.2021
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present invention provides a pharmaceutical composition for treatment of cancer, comprising, as active ingredients, a fusion protein dimer including IL-2 protein or a variant thereof and CD80 protein or a fragment thereof and an immune checkpoint inhibitor. A fusion protein comprising CD80 fragment, immunoglobulin Fc, and an IL-2 variant according to an embodiment of the present invention can activate immune cells such as natural killer cells while controlling the immune cell regulation activity of regulatory T cells. In addition, the administration of an immune checkpoint inhibitor known as an PD-1 inhibitor, such as keytruda, in combination with the fusion protein can effectively inhibit cancer. Therefore, a pharmaceutical composition comprising, as active ingredients, a fusion protein including IL-2 protein or a variant thereof and CD80 protein or a fragment thereof and an immune checkpoint inhibitor can be effectively utilized for the treatment of cancer and thus is of high industrial applicability. La présente invention concerne une composition pharmaceutique pour le traitement d'un cancer, comprenant, en tant que principes actifs, un dimère de protéine de fusion constitué de la protéine IL-2 ou d'un de ses variants et de la protéine CD80 ou d'un fragment de celle-ci ainsi qu'un inhibiteur de point de contrôle immunitaire. Selon un mode de réalisation de la présente invention, une protéine de fusion constituée d'un fragment CD80, d'un Fc d'immunoglobuline et d'un variant IL-2 peut activer des cellules immunitaires telles que des cellules tueuses naturelles tout en contrôlant l'activité de régulation des cellules immunitaires des lymphocytes T régulateurs. De plus, l'administration d'un inhibiteur de point de contrôle immunitaire désigné en tant qu'inhibiteur de PD-1, tel que le keytruda, en combinaison avec la protéine de fusion peut efficacement inhiber un cancer. Par conséquent, une composition pharmaceutique comprenant, en tant que principes actifs, une protéine de fusion constituée de la protéine IL-2 ou d'un de ses variants et d'une protéine CD80 ou d'un fragment de celle-ci ainsi qu'un inhibiteur de point de contrôle immunitaire peut efficacement être utilisée pour le traitement d'un cancer et est, par conséquent, d'une application industrielle élevée. 본 발명은 IL-2 단백질 또는 이의 변이체 및 CD80 단백질 또는 이의 단편을 포함하는 융합단백질 이량체 및 면역관문 억제제를 유효성분으로 포함하는 암 치료용 약학 조성물을 제공한다. 본 발명의 일 구체예인 CD80 단편, 면역글로불린 Fc 및 IL-2 변이체를 포함하는 융합단백질은 자연살해세포와 같은 면역세포를 활성화시킬 수 있으며, 동시에 조절 T 세포의 면역세포 조절 활성을 제어할 수 있다. 또한, PD-1 억제제로 알려진 키트루다와 같은 면역관문 억제제를 상기 융합단백질과 병용 투여할 경우 암을 효과적으로 억제할 수 있다. 따라서, IL-2 단백질 또는 이의 변이체 및 CD80 단백질 또는 이의 단편을 포함하는 융합단백질 및 면역관문 억제제를 유효성분으로 포함하는 약학 조성물은 암의 치료에 효과적으로 활용할 수 있어 산업적 활용 가능성이 높다.