Dasiglucagon for treating severe hypoglycemia in patients with diabetes.

INTRODUCTION: Diabetic patients are prone to hypoglycemia when treated with insulin. Dasiglucagon is a water-soluble and ready-to-use glucagon analog developed for treating hypoglycemia in patients with diabetes. AREAS COVERED: A comprehensive literature search was conducted in PubMed. Key search terms included dasiglucagon and hypoglycemia. The pharmacological characteristics, clinical evidence, and place in therapy of dasiglucagon were reviewed. EXPERT OPINION: Dasiglucagon is a glucagon analog that is stable in water-soluble formulation. It can increase plasma glucose in a dose-dependent manner. Clinical studies have shown that dasiglucagon rapidly and effectively improved insulin-induced hypoglycemia in patients with diabetes. Dasiglucagon was well tolerated and the common adverse events included nausea and vomiting.

Teprotumumab for the treatment of thyroid eye disease.

INTRODUCTION: Thyroid eye disease is a debilitating, disfiguring, and potentially blinding periocular condition. Teprotumumab is a human insulin-like growth factor-I receptor monoclonal inhibitor antibody which indicated for treating thyroid eye disease. AREAS COVERED: The authors performed a systematic review of the literature using the PubMed database, and the following keywords were used: 'teprotumumab,' 'thyroid eye disease,' and 'insulin-like growth factor I receptor.' The chemical property, mechanism of action, pharmacokinetics, clinical efficacy, and safety of teprotumumab were introduced in this paper. EXPERT OPINION: Teprotumumab is a human monoclonal antibody targeting insulin-like growth factor-I receptor. Clinical trials indicated that proptosis response of teprotumumab was 83%, and clinical activity score, diplopia, and quality of life were also better than placebo. Teprotumumab was well tolerated, common adverse reactions included muscle spasm, nausea, alopecia, diarrhea, fatigue, hyperglycemia, hearing impairment, dysgeusia, headache, and dry skin.

Synthesis and antibacterial evaluation of novel clarithromycin derivatives with C-4″ elongated arylalkyl groups against macrolide-resistant strains.

Novel clarithromycin derivatives with C-4″ elongated arylalkyl groups were designed, synthesized and evaluated to probe the effect of different lengths of their C-4″ side chains on the activity against resistant bacterial strains. These derivatives had excellent activity against erythromycin-susceptible Streptococcus pneumoniae, Streptococcus aureus or Streptococcus pyogenes and some of them exhibited greatly improved activity against erythromycin-resistant strains. Compounds 18 and 16, which had the C-4″ elongated arylalkyl groups with eight atoms from the 4″-oxygen atom to the terminal benzene ring, were the most effective against S. pneumoniae expressing the erm gene and the erm and mef genes. In contrast, the most potent compounds 3, 5, 9, 17 and 18 against S. pneumoniae expressing the mef gene had C-4″ elongated arylalkyl groups with three to eight atoms between the 4″-oxygen atom and the terminal aromatic ring.

Synthesis and antibacterial activity of novel 4''-O-arylalkylcarbamoyl and 4''-O-((arylalkylamino)-4-oxo-butyl)carbamoyl clarithromycin derivatives.

Novel series of novel 4''-O-arylalkylcarbamoyl and 4''-O-((arylalkylamino)-4-oxo-butyl)carbamoyl clarithromycin derivatives were designed, synthesized and evaluated for their in vitro antibacterial activities. These derivatives retained excellent activity against the erythromycin-susceptible strains and showed significantly improved activity against all of the tested erythromycin-resistant strains. Among them, compound 4c was the most effective (0.06 microg/mL) against Streptococcus pneumonia encoded by the erm gene and compound 4a was had the most potent activity (0.25 microg/mL) against S. pneumonia encoded by the erm and mef genes.