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calcifediol (Replidea / JTT 762 / CTAP 101)

✓ Approved

Pharmsynthez · VDR · 小分子

什么是 calcifediol？

calcifediol 是一种小分子，由Pharmsynthez研发。该药已获批，用于治疗相关适应症，给药途径：Injectable (Others)、Intravenous (IV)、Oral (PO)。

药物档案

商品名Replidea, JTT 762, CTAP 101
公司Pharmsynthez
药物类别小分子
分子靶点VDR
给药途径Injectable (Others), Intravenous (IV), Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Pharmsynthez

作用机制

分子靶点

calcifediol 作用于 1 个分子靶点：

VDRvitamin D receptor (NR1I1, PPP1R163)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

calcifediol 针对 5 个适应症，涉及 5 个治疗领域。

治疗领域疾病/病症分期
Endocrine disordersHyperparathyroidism secondary✓ Approved
Metabolism and nutrition disordersVitamin D deficiency✓ Approved
Renal and urinary disordersEnd stage renal disease✓ Approved
Infections and infestationsCOVID-19Phase II
Immune system disordersCytokine release syndromePreclinical

相关研究文献

PubMedMaterials today. Bio2026-09-10

EpCAM aptamer modified carbon@manganese dioxide nanoflower for synergistic drug-nanozyme allergic rhinitis treatment.

Zhang Leichao L, Cong Longying L, Gao Yiyao Y, Zhang Wei W et al.

Allergic rhinitis (AR) is a prevalent upper respiratory allergic disorder that significantly impacts patients' quality of life.In this research, we developed a multifunctional nanozyme-drug synergistic therapy nanosystem for the treatment of allergic rhinitis (AR). The nanosystem, called EpCAM aptamer modified carbon@manganese dioxide nanoflower (Apt-C@MnO2 NFs), combines porous carbon nanospheres and MnO2 nanozymes to achieve synergistic reactive oxygen species (ROS) scavenging. EpCAM aptamer (Apt) is an epithelial cell adhesion molecule. The designed material was modified with EpCAM aptamers, endowing it with prominent targeting capability to epithelial cells. The modification with PEG facilitates the penetration of NFs through mucus more rapidly, and the Apt enables the NFs to specifically target human nasal epithelial cells (HNEPc). In addition, it can effectively load and sustainably release the anti-inflammatory drug budesonide (BUD). In vitro experiment demonstrated the system's ability to target HNEPc, deliver drugs, exhibit multi-enzyme activity, and regulate inflammatory factors. In vivo studies in mice showed that Apt-C@MnO2 NFs could restore the expression of mitochondrial biogenesis-related proteins, reduce inflammatory cell infiltration, regulate inflammatory pathways, and alleviate AR symptoms. The research provides a new approach for AR therapy, offering a multifunctional system with significant anti-inflammatory effects and imaging tracking capabilities. This innovative therapeutic strategy combines nanozyme technology with targeted drug delivery to achieve effective treatment of AR.

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Engineered hollow Prussian blue nanoparticles for synergistic anti-inflammatory therapy in sepsis.

Song Yang Y, Yu Xue X, Wu Mingzhe M, Liu Jing J et al.

Sepsis is a systemic inflammatory response triggered by pathogenic infections, often accompanied by bacterial endotoxin release, accumulation of cell-free DNA (cfDNA), and excessive inflammatory reactions, leading to organ failure. Conventional antibiotic therapies are often inadequate in effectively eliminating pathogens and their toxic components, and fail to suppress the cfDNA-mediated inflammatory cascade. In this study, we developed a multifunctional nanotherapeutic platform based on hollow Prussian blue nanoparticles (HPB-NPs) loaded with polymyxin E (PME) and surface-modified with polyethylenimine (PEI). This versatile nanosystem (HPB-NPs@PME@PEI) exhibits potent antimicrobial activity against Gram-negative bacteria and specifically neutralizes lipopolysaccharides (LPS); PEI captures elevated levels of LPS and cfDNA in septic blood via electrostatic adsorption, thereby blocking its activation of the TLR4/MyD88 pathway and mitigating the cytokine storm; meanwhile, HPB scavenges reactive oxygen species (ROS), alleviating oxidative stress damage. Experimental results demonstrate that HPB-NPs@PME@PEI significantly reduces plasma cfDNA levels, suppresses the release of pro-inflammatory cytokines, and improves survival rates in a murine sepsis model. HPB-NPs@PME@PEI directly suppress LPS-induced inflammatory activation and NETosis in innate immune cells. Furthermore, by scavenging ROS and blocking the TLR4/MyD88/NF-κB pathway, HPB-NPs@PME@PEI effectively protects lung and renal epithelial cells from LPS injury. Thus, the nano-system operates via a synergistic mechanism, concurrently neutralizing LPS, clearing ROS, and inhibiting a major inflammatory signaling cascade.

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A three-session webinar series was held by the IQ Consortium in early May 2023 on the topic of in vitro release testing of long acting injectable and parenteral (non-oral) drug products. Attendance was excellent, indicating the high level of interest in this topic. This paper provides a high-level overview of the talks that were given during the webinar and the open discussion session.

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Pyridoxal-phosphate-dependent biosynthesis of aminovaleramide by AvaS in tRNA.

Sun Jingjing J, Wu Junzhou J, Yuan Yifeng Y, Balamkundu Seetharamsing S et al.

In eubacteria, decoding of isoleucine codon AUA requires a specialized tRNA (tRNAIle2) modified with lysidine (k2C) at the anticodon wobble position (C34), which switches decoding specificity from methionine (AUG) to isoleucine (AUA). Recently, aminovaleramide cytidine (ava2C) was discovered at the same tRNA position in several bacteria and plants and shown to support AUA decoding and Ile-specific aminoacylation. However, the enzyme catalyzing ava2C was unknown. Here, we report that tRNAIle-aminovaleramididine synthetase (AvaS) catalyzes ava2C biosynthesis in Pseudomonas aeruginosa PA14. AvaS converts k2C to ava2C through a pyridoxal-phosphate-dependent oxidative decarboxylation mechanism, supported by site-directed mutagenesis and in vitro enzymatic assays. Dual-reporter assays demonstrated that ava2C-modified tRNA exhibits lower AUA decoding efficiency than k2C-modified tRNA. Additionally, genome-wide screening revealed an unexpected link between ava2C levels and metabolic and stress response pathways influencing i6A/ms2i6A dynamics. Together, these findings define the molecular basis of ava2C biosynthesis and its broader cellular metabolic networks.

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Yasmin Adeela A, Casula Luca L, Pittiu Alessio A, Massoni Claudia C et al.

Introduction: Chronic wounds represent a major clinical challenge due to their complex pathophysiology, characterized by persistent inflammation, excessive production of reactive oxygen species (ROS), high risk of microbial contamination, and impaired tissue regeneration. Despite several plant extracts offering antioxidant, anti-inflammatory, and antibacterial properties, their therapeutic use is limited by poor stability and rapid clearance of the active compounds from the wound site, particularly in the case of hydrophilic molecules. In this study, a verbascoside-rich extract obtained from Buddleja davidii was encapsulated into liposomes for potential wound healing applications. Methods: The formulations were characterized in terms of vesicle size, polydispersity index, and zeta potential using dynamic and electrophoretic light scattering. Encapsulation efficiency and verbascoside release profiles were assessed by HPLC, while antioxidant activity was evaluated by the DPPH assay. Formulation stability was monitored for two months, and in vitro biocompatibility and antioxidant protective effects were investigated in human keratinocytes, while antimicrobial activity was tested against methicillin-resistant Staphylococcus aureus (MRSA) and Escherichia coli. Results: The liposomal formulations modulated the release kinetics of verbascoside, showing a prolonged release of the encapsulated fraction, limiting its rapid dispersion in aqueous environments and enabling sustained availability over time. Encapsulation preserved the antioxidant activity of the extract and ensured excellent in vitro biocompatibility across a wide concentration range. Finally, liposomes showed strong and concentration-dependent antimicrobial activity against MRSA, as well as bacteriostatic responses against E. coli. Discussion: Collectively, these findings highlight liposomal encapsulation as a solid strategy to prolong the release-and thus the residence time-of hydrophilic plant-derived actives while maintaining or potentiating their biological activities in the context of wound healing.

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Sun Yuqing Y, Bao Jiangkai J, Li Jialin J, Xie Siwen S et al.

Water stress presents a critical threat to the advancement of global sustainable development. With the advantages of low-carbon operation and high efficiency, solar-driven interfacial evaporation has emerged as a highly promising technology. However, the inherent intermittency of solar energy severely limits its continuous operation and practical application. To achieve this goal, this work proposes an innovative design strategy of matrix stabilization-functional encapsulation, constructing a functionally integrated "energy storage core-evaporation shell" core-shell structure evaporator. This evaporator employs an inner composite phase-change aerogel as its thermal management core, enabling controlled heat storage and release. The outer layer utilizes polypyrrole (PPy)-modified hydrophilic nonwoven fabric to simultaneously achieve favorable photothermal conversion and rapid directional water transfer. Consequently, the thermal management pathway and water transport pathway are synergistically optimized, effectively resolving issues such as insufficient coupling between thermal and water pathways. Experiments demonstrate that this evaporator achieves 97% solar absorption efficiency, with an evaporation rate of 2.22 kg m-2 h-1 and a photothermal conversion efficiency of 96.04%. Even after illumination ceases, the system can sustain evaporation at a rate of 0.92 kg m-2 h-1 for 1 h, a process driven by latent heat released from phase-change materials. This enables the evaporation process to extend from illuminated periods to nonilluminated periods. Furthermore, the evaporator demonstrates outstanding stability and purification performance in various complex water environments. Through synergistic structural and material design, this work achieves efficient integration of energy storage units with an evaporation interface.

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