BIOCHEMISTRY, BIOMEDICINE & PHARMACEUTICS

Nivolumab a-k-a OPDIVO is a FDA-approved checkpoint inhibitor drug for the treatment of a subset of cancer types.  It is a human monoclonal antibody that blocks the interaction between PD-1 and its ligands, PD-L1 and PD-L2. Nivolumab is an IgG4 kappa immunoglobulin that has a calculated molecular mass of 146 kDa. It is expressed in a recombinant Chinese Hamster Ovary (CHO) cell line.  Indication of Nivolumab Immunotherapy Nivolumab (OPDIVO) is a programmed death receptor-1 (PD-1) blocking antibody indicated for the treatment of:  Patients with BRAF V600 wild-type unresectable or metastatic melanoma, as a single agent.   Patients with BRAF V600 mutation-positive unresectable or metastatic melanoma, as a single agent. Patients with unresectable or metastatic melanoma, in combination with ipilimumab. Patients with melanoma with lymph node involvement or metastatic disease who have undergone complete resection, in the adjuvant setting. Patients with meta...

TOPAMAX (topiramate), FDA Approved Drug For the Treatment of Epilepsy Topiramate is a sulfamate-substituted monosaccharide. TOPAMAX (topiramate). Topiramate is designated chemically as 2,3:4,5­ Di-O-isopropylidene-beta-D-fructopyranose sulfamate. TOPAMAX (topiramate capsules) Sprinkle Capsules are available as 15 mg and 25 mg sprinkle capsules for oral administration as whole capsules or opened and sprinkled onto soft food. Indication of TOPAMAX TOPAMAX (topiramate) is indicated for:  Monotherapy epilepsy: Initial monotherapy in patients with & above 2 years of age with partial-onset or primary generalized tonic-clonic seizures    Adjunctive therapy epilepsy: Adjunctive therapy for adults and pediatric patients (2 to 16 years of age) with partial-onset seizures or primary generalized tonic-clonic seizures, and in patients with and above 2 years of age with seizures associated with Lennox-Gastaut syndrome (LGS) ( Migraine: Treatment for adults and adolescen...

Anifrolumab is the FDA approved antibody therapy for Systemic Lupus Erythematosus Anifrolumab-fnia is a type I interferon (IFN) receptor antagonist, immunoglobulin G1 kappa (IgG1κ) monoclonal antibody that is produced in mouse myeloma cells (NS0) by recombinant DNA technology. The molecular weight is approximately 148 kDa.  Indication of SAPHNELO/Anifrolumab: SAPHNELO is a type I interferon (IFN) receptor antagonist indicated for the treatment of adult patients with moderate to severe systemic lupus erythematosus (SLE), who are receiving standard therapy. Limitations of Use:  The efficacy of SAPHNELO has not been evaluated in patients with severe active lupus nephritis or severe active central nervous system lupus. The use of SAPHNELO is not recommended in these situations. Contraindications SAPHNELO is contraindicated in patients with a history of anaphylaxis with anifrolumab-fnia Warning and Precautions Serious Infections: Serious and sometimes fatal infections have occu...

Immune checkpoint inhibiting immunotherapies: These are the class of monoclonal antibody therapies that prevents T-cell inhibition and promotes the activation and proliferation of effector T cells. Two such receptors CTLA-4 & PD-1 that are expressed in T cells transduce inhibitory signals after binding to its ligand.  The monoclonal antibodies targeted against these receptors or their ligands have been shown to increase the tumor-killing activity of T cells.  Figure 1: Immune Check Point Inhibiting Monoclonal Antibodies and its Target in T cells and Tumors. Pembrolizumab (Keytruda), Nivolumab (Opdivo), and cemiplimab (Libtayo) block PD-1 expressed in T cells. Atezolizumab (Tecentriq), Avelumab (Bavencio), and Durvalumab (Imfinzi) block PD-L1 expressed in tumor cells. Ipilimumab (Yervoy) blocks CTLA-4 antigen present in T cells   PD-1 inhibiting antibodies:  These monoclonal antibodies block the PD-1 signaling by binding to its ligand PD-1 expressed i...