Pfizer’s PF-06482077 is a 20-valent pneumococcal conjugate vaccine, which is currently in Phase II development in the US and EU. PF-06482077 contains the 13 serotypes included in Prevnar 13 (4, 6B, 9V, 14, 18C, 19F, 23F, 1, 3, 5, 6A, 7F, and 19A), as well as seven additional serotypes.
An oral antiplatelet agent, Effient is a pro-drug which is converted to its active metabolite after metabolism by cytochrome P450 enzymes.
Taltz (ixekizumab; Eli Lilly/Torii Pharmaceutical) is a humanized, immunoglobulin G subclass 4 monoclonal antibody that neutralizes interleukin-17.
Aliqopa (copanlisib; Bayer) is a small molecule phosphoinositide 3-kinase (PI3K) inhibitor with high selectivity for the p110-alpha/delta catalytic subunits. The PI3K pathway is crucial for normal B-cell development, and is subverted by follicular lymphoma (FL) to promote survival and growth.
Lefitolimod is a synthetic DNA-based immunomodulator that acts as a Toll-like receptor (TLR)9 agonist.
Adempas (riociguat; Bayer/Merck & Co) is a first-in-class drug that activates soluble guanylyl cyclase (sGC), a key enzyme in nitric oxide-mediated vasodilation of vascular smooth muscle cells.
Aubagio is the major active metabolite of Arava (leflunomide), Sanofi’s oral treatment for rheumatoid arthritis, and is a dihydroorotate dehydrogenase (DHODH) inhibitor.
Pfizer developed Zyvox (linezolid) as the first oxazolidinone antimicrobial agent. The drug gained its first regulatory approval for the treatment of complicated skin and skin structure infections (cSSSI) in the US market in 2000.
Finerenone (Bayer) is a third-generation potent and selective oral, non-steroidal mineralocorticoid receptor antagonist (MRA). It blocks the detrimental effects due to over-activation of the receptor.
Selonsertib (Gilead) is a small molecule that inhibits apoptosis signal-regulating kinase 1 (ASK1). ASK1 has been shown to promote inflammation, apoptosis, and fibrosis in settings of oxidative stress. Non-alcoholic steatohepatitis (NASH) increases oxidative stress and ASK1 activation, so by inhibiting ASK1, selonsertib has been shown to decrease inflammation and fibrosis in patients with NASH.
While PT003 (formoterol/glycopyrrolate; AstraZeneca) demonstrated statistically significant
improvements in trough forced expiratory volume in one second (FEV1) compared to its individual
components and placebo in its Phase III PINNACLE program, pulmonologists are unconvinced about its
role in symptom improvement.
Launching after Revatio, Adcirca became the second-to-market PDE5 inhibitor upon its approval in major markets in 2009. Inhibiting the PDE5 enzyme enhances the effect of the endogenous vasodilator, nitric oxide (NO).
Lusefi (luseogliflozin; Taisho) is a member of the novel sodium-glucose cotransporter-2 (SGLT-2) inhibitor class.
Lonasen (Sumitomo Dainippon/Nitto Denko) contains blonanserin, a dopamine D2 and serotonin 5-HT2 receptor antagonist.
Vasotec’s (enalapril; Merck & Co/Valeant) role in chronic heart failure (CHF) is severely limited by
competition from generic equivalents.
Simponi (golimumab; Johnson & Johnson/Merck & Co/Mitsubishi Tanabe) is a second-generation TNF inhibitor following Johnson & Johnson’s Remicade (infliximab).
Trimbow ([beclomethasone + formoterol + glycopyrrolate]; Chiesi Farmaceutici) is a fixed triple-combination product consisting of glycopyrrolate (a LAMA), formoterol (a LABA), and beclometasone (an ICS), used to relieve the symptoms of moderate to severe chronic obstructive pulmonary disease (COPD).
Gantenerumab (Roche/MorphoSys) is a fully humanized centrally and N-acting monoclonal antibody that primarily targets fibrillar amyloid-beta.
SPK-9001 is Spark Therapeutics’ leading candidate in development for hemophilia B.
Atripla (efavirenz/emtricitabine/tenofovir disoproxil fumarate [TDF]; Gilead/Bristol-Myers Squibb) is a single-tablet regimen approved for the treatment of HIV-1 infection.
Avonex is a biological therapy derived from the interferon family, and Biogen’s leading drug for treating relapsing-remitting multiple sclerosis (RRMS).
Apalutamide (Johnson & Johnson) is an orally available androgen signaling inhibitor. The drug exhibits high binding affinity to the ligand-binding domain of androgen receptor (AR) and subsequently inhibits its nuclear import, as well as its ability to bind to DNA. Apalutamide has a similar mechanism of action to Xtandi (enzalutamide; Pfizer/Astellas).
Complera (rilpivirine/emtricitabine/tenofovir disoproxil fumarate [TDF]; Gilead/Johnson & Johnson) is a single-tablet regimen for the treatment of HIV-1 infection.
Following its 2010 launch, Sorilux (calcipotriene; Stiefel/GlaxoSmithKline) has experienced slow
uptake in the psoriasis market, despite having the financial support of GlaxoSmithKline. This comes as
no surprise as the US psoriasis market is saturated with several types of established calcipotriene
formulations, limiting Sorilux’s uptake.
Asciminib (Novartis) is a BCR-ABL-targeted tyrosine kinase inhibitor (TKI) in development by Novartis for Philadelphia chromosome-positive diseases such as chronic myeloid leukemia (CML) and acute lymphoblastic leukemia.
Lu AF35700 (Lundbeck) has a novel pharmacological profile as a dopamine D1 and D2 antagonist with a high occupancy of 5-HT2A and 5-HT6 serotonin receptors.
Evinacumab (Regeneron) is a monoclonal antibody (MAb) that inhibits angiopoietin-like 3 inhibitor (ANGPTL3). ANGPTL3 is secreted naturally by the liver and acts as a partial inhibitor of lipoprotein lipase and endothelial lipase.
Farxiga (dapagliflozin; AstraZeneca) is a member of the novel sodium-glucose cotransporter-2 (SGLT-2) inhibitor class.
Faslodex (fulvestrant; AstraZeneca) is an analog of 17 beta-estradiol, the dominant circulating estrogen, which competitively inhibits the binding of natural estradiol to the estrogen receptor (ER).
Entrectinib (Roche/Chugai/Nerviano) is a selective tyrosine kinase inhibitor (TKI) of the tropomyosin receptor kinases (Trk) A, B, and C; ROS1; and anaplastic lymphoma kinase (ALK) proteins. Under normal conditions, these oncogenes regulate the flow of cellular growth signaling.
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