Nanjing Chia Tai Tianqing Pharmaceutical Co. Ltd. has disclosed bifunctional compounds acting as RAC serine/threonine-protein kinase (AKT; PKB) degraders reported to be useful for the treatment of cancer.
Receptor tyrosine kinase-like orphan receptor 1 (ROR1), a receptor tyrosine kinase activated by Wnt5, is mainly expressed during fetal development and plays a crucial role in processes such as neurodevelopment and angiogenesis. ROR1 is nearly absent in most adult and pediatric tissues but is overexpressed in various malignancies, including leukemia and lung and breast cancers. Its expression has been correlated with poor clinical outcomes, and therefore, it is considered a promising cancer therapeutic target.
Targeting SHP2 has emerged as a promising approach for treating cancers driven by receptor tyrosine kinases. Although allosteric SHP2 inhibitors have shown strong antitumor activity in preclinical studies, their clinical efficacy as monotherapies has been limited. Recent studies indicate that combining SHP2 inhibitors with kinase inhibitors may enhance treatment effectiveness and help overcome therapeutic resistance.
China has proved to be a fertile ground for innovation as evidenced by some big deals in the antibody-drug conjugate (ADC) space, and the number of candidates entering clinical trials in China or being advanced in the U.S. by Chinese companies.
Actithera A/S is poised to bring small-molecule pharmacokinetics to radiopharmaceuticals after closing a $75.5 million series A that will fund initial clinical development of a candidate targeting the elusive fibroblast activation protein (FAP).
Researchers at the Chinese Academy of Sciences and collaborators have developed a new method to label and monitor dormant breast cancer cells over time, shedding light on how these cells survive chemotherapy and potentially trigger metastatic relapse in the lung. Breast cancer frequently recurs in distant metastatic sites, even after the primary tumor has fully regressed following initial therapy.
China’s National Medical Products Administration gave the green light to Simcere Pharmaceutical Group Ltd.’s Enzeshu (suvemcitug) for treating recurrent ovarian cancer, fallopian tube cancer, or primary peritoneal cancer in combination with paclitaxel, liposomal doxorubicin, or topotecan in adults who have received at least one systemic therapy after platinum resistance.
Four days ahead of its July 7 PDUFA date, the U.S. FDA granted accelerated approval to Dizal (Jiangsu) Pharmaceutical Co. Ltd.’s sunvozertinib (DZD-9008), branded as Zegfrovy, for treating adults with locally advanced or metastatic non-small-cell lung cancer with epidermal growth factor receptor exon 20 insertion mutations following platinum-based chemotherapy.
Aussie researchers have used CRISPR gene editing tools to “armor” chimeric antigen receptor (CAR) T cells to activate additional cancer-fighting proteins at the tumor site, enabling them to target cancer cells in solid tumors.
Degradation is a therapeutic strategy that could offer possibilities to get at currently undruggable target proteins. In targeted degradation, compounds induce interactions between a target protein and a protein that can tag the target for degradation. In principle, there are several pathways that could be used for such tagging; the most attention has gone to ubiquitin ligases, in particular cereblon, a protein that is part of a ubiquitin ligase complex and the target of several approved drugs.
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