Database for
Therapeutic Antibodies
Therapeutic Antibodies
| Entry ID | 1712 |
| INN | Trastuzumab botidotin |
| Status | Regulatory review |
| Drug code(s) | A166, 博度曲妥珠单抗 |
| Brand name | 舒泰萊® |
| mAb sequence source | mAb humanized |
| General Molecular Category | ADC |
| Format, general category | Full length Ab conjugate |
| Format details | None |
| Isotype (Fc) | IgG1 |
| Light chain isotype | kappa |
| Linker | Valine-Citrulline, Cleavable linker |
| Ave. DAR | 2, Site-specific |
| Conjugated/fused moiety | Tubulin inhibitor, Duostatin-5 |
| Discovery method/technology | None |
| Target(s) | HER2 |
| Indications of clinical studies | Solid tumors |
| Primary therapeutic area | Cancer |
| Most advanced stage of development (global) | Regulatory review China |
| Status | Active |
| Start of clinical phase (IND filing or first Phase 1) | July 16, 2018 |
| Start of Phase 2 | October 15, 2021 |
| Start of Phase 3 | July 15, 2023 |
| Date BLA/NDA submitted to FDA | |
| Year of first approval (global) | None |
| Date of first US approval | |
| INN, US product name | None |
| US or EU approved indications | None |
| Company | Kelun-Biotech, subsidiary Klus Pharma |
| Licensee/Partner | Sorrento Therapeutics, Inc. |
| Comments about company or candidate | June 2024: Stil in review (https://www1.hkexnews.hk/listedco/listconews/sehk/2024/0819/2024081901322.pdf) China marketing application acceptance date is May 11, 2023, sponsor is Sichuan Kelun-Biotech Biopharmaceutical Co Ltd according to NMPA's CDE database. Phase 3 study for HER2-positive unresectable or metastatic breast cancer (CTR20231740) started in July 2023. Pivotal phase 2 CTR20212088 for breast cancer status is "In progress Recruitment completed". CTR20212088 Phase 2 pivotal study is ongoing in China as per company website accessed Feb 2023 (https://www.kluspharma.com/pipeline) NCT03602079 Phase 1/2 study active not recruiting as of last update in Feb 2022; NCT05346328 Phase 2 study sponsored by Fudan University due to start in June 2022. June 04, 2021 Sorrento Therapeutics, Inc. announced that Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. (“Kelun”), a license and development partner, will present posters at this year’s American Society of Clinical Oncology (ASCO) meeting to be held June 5-6, 2021, releasing Phase 1 data for its HER2-ADC, A166. To generate this site-specific third generation antibody drug conjugate (ADC), Kelun partnered with Levena Biopharma, a wholly owned subsidiary of Sorrento, which provided the patent-protected technologies for the generation and production of A166, including (1) a proprietary small molecule toxin, Duostatin-5, a tubulin inhibitor, (2) K-Lock, a site-specific conjugation technology and (3) an enzymatically cleavable linker. Compared to its commercial competitors, A166 demonstrated a better safety profile in the initial study and potentially better efficacy, as shown in the overall response rate (ORR) of 71.4% (A166) at 6.0 mg/kg vs DS-8201, which has an ORR of 60.9% (DS-8201) at 5.4 mg/kg. J Clin Oncol 39, 2021 (suppl 15; abstr 1024) DOI:10.1200/JCO.2021.39.15_suppl.1024 Clinical Trial Registry Number: CTR20181301 NCT03602079 is a Phase I-II, FIH Study of A166 in Locally Advanced/Metastatic Solid Tumors Expressing Human Epidermal Growth Factor Receptor 2 (HER2) or Are HER2 Amplified That Did Not Respond or Stopped Responding to Approved Therapies; started in July 2018, this study is still recruiting patients as of Aug 2019. Klus Pharma is a US subsidiary of Kelun Pharmaceuticals, which is based in China. |
| Full address of company | 101 College Rd East, 2F, Princeton Forrestal Center, Princeton, NJ 08540 North America United States of America https://www.kluspharma.com/contact |
2021: A166 (ASCO Abstract #1024) is a third generation antibody drug conjugate (ADC) against HER2-positive breast cancer with Levena’s proprietary tubulin inhibitor Duo-5 toxin, cleavable linker and site-specific K-Lock™ conjugation chemistry.
| Anticipated events | Regulatory review China - anticipate approval second half of 2024 or the first half of 2025 - https://www1.hkexnews.hk/listedco/listconews/sehk/2024/0819/2024081901322.pdf |
| Factor(s) contributing to discontinuation | None |