Title:
RNA INHIBITOR FOR INHIBITING HEPATITIS B VIRUS GENE EXPRESSION AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/218163
Kind Code:
A1
Abstract:
Provided are an RNA inhibitor for inhibiting hepatitis B virus (HBV) gene expression and an application thereof. The RNA inhibitor is formed of a sense strand and an antisense strand by means of base pairing; at least 85% of bases of the sense strand and the antisense strand are complementary to each other; and -OH at position 2' of some or all of nucleotide glycosyl is substituted with fluorine or methoxy, and at terminuses, phosphate esters among at least three consecutive nucleotides are thiolated. In the structure of the RNA inhibitor, 5' MVIP and 3' MVIP are also comprised, such that the RNA inhibitor has specific liver targeting. The RNA inhibitor can continuously inhibit the synthesis of an HBV surface antigen (HBsAg), generates an HBV surface antibody (HBsAb), has an inhibitory effect on all most common types of HBV, i.e., A, B, C and D, and is capable of functionally curing hepatitis B by being used in combination with a nucleoside analog or interferon.
Inventors:
MU ZHUO (CN)
WANG SHENGJUN (CN)
WANG SHENGJUN (CN)
Application Number:
PCT/CN2022/084381
Publication Date:
October 20, 2022
Filing Date:
March 31, 2022
Export Citation:
Assignee:
KYLONOVA XIAMEN BIOPHARMA CO LTD (CN)
International Classes:
C12N15/113; A61K31/713; A61P3/06; A61P3/10; A61P7/00; A61P9/10; A61P9/12; A61P31/20; A61P35/00
Foreign References:
| CN113171371A | 2021-07-27 | |||
| CN110846320A | 2020-02-28 | |||
| CN103333890A | 2013-10-02 | |||
| US20200171069A1 | 2020-06-04 | |||
| CN102140459A | 2011-08-03 |
Other References:
SU LAN; ZHANG PING; WANG YANGJUNQI; ZHONG RUGANG: "Progress on the inhibition of Hepatiti B Virus by sRNA Strategy", ZHONGGUO SHENGWU GONGCHENG ZAZHI - CHINA BIOTECHNOLOGY, ZHONGGUO KEXUEYUAN WENXIAN QINGBAO ZHONGXIN,CHINESE ACADEMY OF SCIENCES, DOCUMENTATION AND INFORMATION CENTER, CN, vol. 34, no. 9, 15 September 2014 (2014-09-15), CN, pages 102 - 105, XP009520827, ISSN: 1671-8135, DOI: 10.13523/j.cb.20140915
ANDREW Z. FIRE ET AL., SCIENCE, 1998
ANDREW Z. FIRE ET AL., SCIENCE, 1998
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