어스바이오는 BLDPharm 한국 공식 대리점입니다.
어스바이오는 BLDPharm 한국 공식 대리점으로서 모든 제품을 전문적으로 취급 및 공급하고 있습니다.
[BLDPharm 한국공식대리점] ARV-471 (Vepdegestrant): a PROTAC Estrogen Receptor Degrader for Breast Cancer
Arvinas and Pfizer are collaborating to develop and commercialize ARV-471, an investigational PROTAC estrogen receptor degrader administered orally for the treatment of patients with estrogen receptor (ER) positive/human epidermal growth factor receptor 2 (HER2) negative (ER+/HER2-) locally advanced or metastatic breast cancer. This program is currently in Phase 3 clinical studies.
Preclinical studies of ARV-471 have been published. It has better tumor inhibition effect compared with ER antagonist Fulvestrant, and oral, daily dose of ARV-471 inhibited tumor growth by 99% at 10 mpk and 106% at 30 mpk in an ESR1 mutant PDX model.
The individual ER and CRBN: DDB1 components were mixed in excess and incubated with Vepdegestrant (green line) and without Vepdegestrant (blue line), then separated using size-exclusion chromatography the size-exclusion. The results were shown in figure, which verified the formation of a ternary complex in the degradation mechanism of PROTAC.
Phase 2 clinical data of ARV-471 were published in November 2022, the CBR(CR+PR+ SD≥24w) of the primary endpoint for the ESR1 mutation subgroup was as high as 51%, and the PFS of the ESR1 mutation subgroup was 5.7 months. Safety studies showed that ARV-471 was well tolerated at both doses, and the most common (≥10%) TRAEs were nausea (27%), fatigue (20%), and vomiting (10%), all of which were grade 1.
어스바이오(USBIO)는 BLDPharm 한국 공식 대리점입니다.
해당 제품에 대한 문의나 BLDPharm 제품의 견적 또는 문의사항이 있으시면 아래로 연락주시기 바랍니다.
Tel: 02-862-2816 / Email: bio@usbio.co.kr
