Croton L. (Euphorbiaceae) is recognized as one of the richest botanical sources of structurally diverse diterpenoids with a remarkable range of biological activities. These compounds display an exceptional diversity of carbon skeletons, many of which are unique to this genus, with bioactivity profiles that make them privileged scaffolds for drug discovery and development. Between 2019 and 2025, research on Croton phytochemistry has expanded considerably, with 40 species reported to contain diterpenoids and 330 new compounds described. This review covers the classification of structural types, plant sources, extraction and isolation techniques, structure elucidation methods, and pharmacological profiles. The newly identified metabolites belong to 14 structural classes, with clerodanes, labdanes, and phorbol esters being the most abundant, particularly in species such as Croton crassifolius Geiseler, Croton damayeshu Y.T. Chang, Croton kongensis Gagnep., Croton tiglium L., and Croton laui Merr. F.P. Metcalf. Clerodane diterpenoids showed the greatest chemical diversity, while kaurane and phorbol esters displayed potent activity in individual assays; yet varying conditions prevent a general potency ranking across classes. Overall, biological evaluations were predominantly conducted in vitro and identified cytotoxic effects against cancer cell lines, anti-inflammatory and antiparasitic activities, and effects in experimental models of metabolic dysfunction and neuronal injury. The compiled data highlight significant advances in diterpene discovery within the genus while also emphasizing current limitations, such as scarce mechanistic studies, very limited in vivo validation, and limited quantities available for testing. These findings lay the groundwork for future research in biosynthesis, chemical synthesis, pharmacology, and biotechnological production to determine the therapeutic potential of Croton-derived diterpenoids.
Edible and medicinal mushrooms are important sources of novel bioactive natural products, abundant in terpenoids, sterols, alkaloids, peptides, and other bioactive substances. These compounds exhibit a variety of physiological functions, including neuroprotective, hepatoprotective, antioxidant, and antitumor properties. The exploration and discovery of novel bioactive components from mushrooms are not only of great significance to the field of functional foods, but also hold tremendous potential for innovative drug development. These novel active ingredients provide new perspectives and resources for modern medicine, health preservation and wellness. In this review, we present a comprehensive summary of 139 novel mushroom-derived bioactive compounds with anti-inflammatory, antibacterial, antimalarial, neuroprotective, antitumor, antioxidant, and enzyme inhibitory activities, as reported in 35 publications over the past two years (September 2024 to August 2026). These compounds, encompassing terpenoids (sesquiterpenoids, diterpenoids, triterpenoids, and meroterpenoids), alkaloids, peptides, lipids, and others, are sourced from diverse mushroom species, with particular focus on their structural characteristics and biological activities. The objective of this review is to provide valuable insights that may facilitate the research and development of novel bioactive natural products of mushroom origin.
Dermatomyositis is a rare systemic autoimmune disease characterized by chronic inflammation, progressive muscle weakness, and prominent cutaneous manifestations, with limited approved treatment options. Brepocitinib (Lisraya®), an orally administered dual tyrosine kinase 2 (TYK2) and Janus kinase 1 (JAK1) inhibitor, received the U.S. Food and Drug Administration approval on August 27, 2026, for the treatment of dermatomyositis in adults. Unlike broader JAK inhibitors, brepocitinib exhibits preferential activity against JAK1 and TYK2 over JAK2 and JAK3, providing a differentiated kinase-selectivity profile. In the phase 3 VALOR trial, once-daily brepocitinib 30 mg significantly improved the Total Improvement Score and multiple measures of dermatomyositis disease activity compared with placebo. Its approval highlights the successful application of kinase-directed medicinal chemistry to a rare autoimmune disease and provides a new oral therapeutic option for adults with dermatomyositis.
Remibrutinib (Rhapsido®) is a selective, orally bioavailable covalent inhibitor of Bruton’s tyrosine kinase (BTK), approved in 2025 for the treatment of adult chronic spontaneous urticaria (CSU) uncontrolled by H1-antihistamines. By blocking BTK, it suppresses signaling pathways driving mast cell, basophil, and B-cell activation in immune-mediated disease. This review traces remibrutinib’s journey from target validation to market approval, detailing the structure–activity relationships that optimized early CGI-560 and CGI-1746 scaffolds into pyrrolopyrimidine and 6-aminopyrimidine series, as well as the process chemistry redesign for commercial synthesis. By covalently capturing BTK in its inactive conformation, remibrutinib achieves exceptional kinase selectivity. This translates into rapid symptom control, convenient oral administration as an alternative to injectable biologics, and a favorable safety profile where mild mucocutaneous bleeding is the primary mechanism-based risk. Remibrutinib is also in late-stage development for other chronic, non-lethal inflammatory conditions including chronic inducible urticaria, hidradenitis suppurativa, Sjögren disease, and multiple sclerosis.
Hormone receptor (HR)-positive and human epidermal growth factor receptor 2 (HER2)-negative tumors are the most common types of breast cancer. Mutation of ESR1 complicates their therapy. On September 04, 2026, camizestrant (Etcamah®) received approval for HR-positive and HER2-negative, locally advanced or metastatic breast cancer after detecting ESR1 mutation during medication with aromatase and CDK4/6 inhibitors. The mutation was identified through circulating tumor deoxyribonucleic acid, thus representing its first interventional use to guide a therapy switch as part of a clinical study. Camizestrant is a selective estrogen receptor degrader (SERD) and complete antagonist of the estrogen receptor. A dose of 75 mg is taken by mouth once daily concomitantly with a cyclin-dependent kinases 4 and 6 (CDK4/6) inhibitor. In a drug regimen comprising an aromatase inhibitor along with a CDK4/6 inhibitor, a significant improvement in progression-free survival was achieved when the aromatase inhibitor was exchanged for camizestrant. This makes camizestrant a next-generation oral SERD for treating advanced breast cancer.
