May 2021

New Products

• Elexacaftor/tezacaftor/ivacaftor and ivacaftor (Trikafta) contains elexacaftor and tezacaftor, which are cystic fibrosis transmembrane conductance regulator (CFTR) correctors that bind to different sites on the CFTR protein and have an additive effect in facilitating the cellular processing and trafficking of F508del-CFTR to increase the amount of CFTR protein delivered to the cell surface compared to either molecule alone. Ivacaftor potentiates the channel open probability (or gating) of the CFTR protein at the cell surface. The combined effect of elexacaftor, tezacaftor and ivacaftor is increased quantity and function of F508del-CFTR at the cell surface, resulting in increased CFTR activity as measured by CFTR mediated chloride transport. Trikafta is indicated for the treatment of cystic fibrosis in patients ≥ 12 years who have at least one F508del mutation in the CFTR gene. Trikafta tablets are available as a composite pack of 56 morning tablets (containing elexacaftor 100 mg, tezacaftor 50 mg and ivacaftor 75 mg as a fixed-dose combination), and 28 evening tablets (containing ivacaftor 150 mg).
   
• Esketamine (HCl) (Spravato), the S-enantiomer of racemic ketamine, is an antidepressant with a novel mechanism of action. It is a non-selective, non-competitive antagonist of the N‑methyl‑D‑aspartate (NMDA) receptor, an ionotropic glutamate receptor. Evidence within the literature suggests that through NMDA receptor antagonism, esketamine produces a transient increase in glutamate release leading to increases in α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) stimulation and, subsequently, to increases in neurotrophic signaling that restore synaptic function in these brain regions. Esketamine’s primary antidepressant action does not directly involve monoamine, GABA, or opioid receptors. Spravato is indicated for treatment resistant depression (major depressive disorder in adults who have not responded adequately to at least two different antidepressants of adequate dose and duration to treat the current moderate to severe depressive episode). It is to be initiated in conjunction with a newly initiated oral antidepressant. Spravato is contraindicated in patients for whom an increase in blood or intracranial pressure poses a serious risk: patients with known aneurysmal vascular disease (including intracranial, thoracic or abdominal aorta, or peripheral arterial vessels), or patients with known history of intracerebral haemorrhage. It is also contraindicated in patients with hypersensitivity to ketamine. Spravato nasal spray contains esketamine 28 mg/2 actuations (equivalent to 0.2 mL) and is available in a pack size of 1, 2 or 3 single-use devices.
   
• Ofatumumab (Kesimpta) is a recombinant human anti-CD20 monoclonal immunoglobulin G₁ (IgG₁) antibody. It binds to a distinct epitope encompassing both the small and large extracellular loops of the CD20 molecule giving rise to a slow off-rate and high binding affinity. The CD20 molecule is a transmembrane phosphoprotein expressed on B lymphocytes from the pre‑B to mature B lymphocyte stage. The CD20 molecule is also expressed on a small fraction of activated T cells. The binding of ofatumumab to CD20 induces lysis of CD20+ B‑cells primarily through complement-dependent cytotoxicity and to a lesser extent, through antibody-dependent cell-mediated cytotoxicity. Ofatumumab has also been shown to induce cell lysis in both high and low CD20 expressing cells. CD20-expressing T cells are also depleted by ofatumumab. Kesimpta is indicated for the treatment of adults with relapsing forms of multiple sclerosis to delay the progression of physical disability and reduce the frequency of relapse. Kesimpta solution for injection contains ofatumumab 20 mg/0.4 mL and is available in a pack size of 1 prefilled pen.

New Indications

• Enzalutamide (Xtandi) is now indicated for the treatment of patients with metastatic hormone-sensitive prostate cancer.
   
• Fulvestrant (Faslodex) is now indicated for the treatment of postmenopausal women with hormone receptor positive, human epidermal growth factor receptor 2 negative, locally advanced or metastatic breast cancer who have not been previously treated with endocrine therapy.
   
• Inactivated quadrivalent influenza vaccine, split virion (influenza virus haemagglutinin) (Vaxigrip Tetra) is now indicated for the active immunisation of pregnant women and passive protection of infants from birth to less than 6 months of age following vaccination of pregnant women against the two influenza A virus subtypes and two influenza B virus types contained in the vaccine.
   
• Lacosamide (Vimpat, Vimpat Injection) is now indicated as add-on therapy in the treatment of primary generalised tonic-clonic seizures in patients ≥ 4 years with idiopathic generalised epilepsy.
   
• Olaparib (Lynparza Tablets) is now indicated as monotherapy for the treatment of adults with BRCA-mutated (germline and/or somatic) metastatic castration-resistant prostate cancer who have progressed following prior therapy that included a new hormonal agent. BRCA mutation status should be determined by an experienced laboratory using a validated test method.
   
• Omalizumab (rch) (Xolair) is now indicated as add-on treatment in adults ≥ 18 years with severe chronic rhinosinusitis with nasal polyps with inadequate response to intranasal corticosteroids.

New Contraindications

• Levonorgestrel/ethinylestradiol and ethinylestradiol (Seasonique) is now contraindicated with the concomitant use of glecaprevir/pibrentasvir and sofosbuvir/velpatasvir/voxilaprevir.
   
• Melphalan (Alkeran, Alkeran Injection) is now contraindicated during lactation.
   
• Siponimod (Mayzent) should not be administered to patients who in the last 6 months had myocardial infarction, unstable angina pectoris, stroke/transient ischemic attack, decompensated heart failure (requiring in-patient treatment), or New York Heart Association Class III/IV heart failure; or with second-degree Mobitz type II atrioventricular (A-V) block, third-degree A-V block, sino-atrial heart block or sick-sinus syndrome, if they do not have a pacemaker.

This list is a summary of only some of the changes that have occurred over the last month.
Before prescribing, always refer to the full product information.