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Daridorexant Hydrochloride is the API form of daridorexant, a dual orexin‑receptor antagonist for adult insomnia treatment. It blocks orexin‑A and orexin‑B binding to OX1 and OX2 receptors to reduce wake‑promoting signals, helping patients fall asleep and maintain sleep without disrupting normal sleep architecture. It appears as white‑to‑light‑yellow powder with poor water solubility. Its finished‑drug brand name is Quviviq, approved by FDA in 2022 for insomnia characterized by sleep‑onset and sleep‑maintenance difficulties. This molecule attracts growing attention for generic formulation and registration projects worldwide.

RECARBRIO (Relebactam) for Injection is a fixed-dose combination antibiotic indicated for serious Gram-negative infections, including hospital-acquired pneumonia, complicated urinary tract infections, and complicated intra-abdominal infections. Each 1.25 g vial contains imipenem, cilastatin, and ralibactam. Ralibactam protects imipenem from degradation by serine β-lactamases and restores its activity against resistant pathogens. Approved in the US (2019), EU (2020), and launched in China (2020), this Class 4 chemical drug is not yet domestically approved in China. We offer full-process formulation development and technology transfer services, with the sterile ralibactam API currently in the validation stage.

This study aims to develop a novel cocrystal form of Trofinetide to circumvent the existing crystalline patent (valid until 2042). The research begins with comprehensive solid-state and solubility characterization of the starting material, followed by computational prediction of pharmaceutically acceptable cocrystal ligands. Systematic screening is performed using both dry and solvent-based methods, including grinding, slurry, and evaporation techniques. Promising cocrystals are optimized, characterized by PXRD, DSC, TGA, and DVS, and evaluated for stability under stress conditions. Additionally, single-crystal cultivation is pursued to confirm the cocrystal structure. The total project duration is estimated at six months.

Merck, in collaboration with Huanquan and Conquer Biotech, publicly disclosed the total synthesis of MK-0616, a first-in-class oral macrocyclic peptide PCSK9 inhibitor for cardiovascular disease. Facing structural complexity, the team developed a scalable route through multi-generation optimization—reducing steps from 63 to 43 and linear sequence from 28 to 21 steps. Key innovations include biocatalysis (KRED, TrpB, hydroxylase), crystallization-driven purification (avoiding chromatography), and orthogonal protecting group strategies. The second-generation process achieves nearly 1,000-fold yield improvement, enabling ton-scale production while significantly lowering costs, setting a benchmark for complex macrocyclic peptide synthesis.

The selection of chelating agents for targeted radionuclides is a precision science centered on matching the radionuclide, chelator, and targeting vector. Classic macrocyclic agents like DOTA offer exceptional stability for medium-sized radionuclides such as ¹⁷⁷Lu, and are used in approved drugs like Lutathera and Pluvicto. For larger α-emitting isotopes like ²²⁵Ac, novel chelators such as Macropa exhibit "reverse size selectivity" for superior complexation. Bifunctional design enables covalent linkage to antibodies or peptides, while high in vivo stability is critical for safety. Emerging research, including dual-size-selective chelators, is paving the way for integrated theranostic applications.

Eutectic technology is an innovative drug development strategy that optimizes the physicochemical properties of active pharmaceutical ingredients (APIs) without altering their chemical structure. By forming co-crystals with suitable ligands, this approach enhances solubility, stability, and bioavailability, enabling synergistic therapeutic effects and reducing toxicity. It also offers a practical pathway to bypass patent barriers, as co-crystals can qualify as novel entities for patent protection. Notably, the FDA may classify co-crystal products containing already-approved APIs as new dosage forms under Section 505(b)(2), potentially streamlining clinical trial requirements. Successful examples like Novartis’ Entresto demonstrate the technology’s substantial commercial potential.