DDInter1042 DDInter1376
Leuprolide is a synthetic 9-residue peptide analogue of gonadotropin-releasing hormone (GnRH). Unlike the endogenous decapeptide GnRH, leuprolide contains a single D-amino acid (D-leucyl) residue, which helps to increase its circulating half-life from three to four minutes to approximately three hours. As a GnRH mimic, leuprolide is capable of binding to the GnRH receptor (GnRHR) and inducing downstream modulation of both gonadotropin hormone and sex steroid levels. Prolonged activation of GnRHR results in significant downregulation of sex steroid levels, which is primarily responsible for the clinical efficacy of leuprolide in diverse conditions, including advanced prostate cancer, endometriosis, and central precocious puberty.[A203126, A203132] Leuprolide was first approved in 1985 as a daily subcutaneous injection under the tradename
Ozanimod is a once-daily sphingosine 1-phosphate receptor modulator for the treatment of relapsing Multiple Sclerosis (MS) and inflammatory bowel disease. It was developed by Celgene (now acquired by Bristol-Myers Squibb) and was approved by the FDA on March 26, 2020.[L12573,L12582] The US approval was followed by the approval in Canada on October 2, 2020. In November 2021, ozanimod was also approved by the European Commission for the treatment of adults with relapsing remitting multiple sclerosis.[L39377,L39382] MS is a devastating inflammatory disease that often progresses and causes severe neurological, physical, and cognitive effects. Inflammatory bowel disease also a chronic inflammatory condition and can cause persistent abdominal pain, diarrhea, bloody stools, and vomiting. In clinical trials, Ozanimod has been shown to be well-tolerated and has resulted in a higher decrease in the rate of MS relapses than with intramuscular [interferon beta-1a], a current standard in MS therapy. Studies involving patients with inflammatory bowel disease have also shown promising results.[A189318,A189342]