SAGE-217 (oral brexanolone; SAGE Therapeutics/Shionogi) is a novel, next-generation positive allosteric modulator that selectively binds synaptic and extrasynaptic gamma-aminobutyric acid-A (GABA-A) receptors and shares similar pharmacology properties to brexanolone.
Zulresso is SAGE Therapeutics’ proprietary intravenous formulation of brexanolone, which is an allosteric modulator of both synaptic and extra-synaptic GABA-A receptors.
Fotivda (tivozanib; AVEO Oncology/EUSA Pharma/Kyowa Hakko Kirin) is an oral tyrosine kinase inhibitor targeting vascular endothelial growth factor receptor 1 (VEGFR-1), VEGFR-2, and VEGFR-3. Inhibition of VEGF signaling in order to prevent angiogenesis is a well-established strategy across many tumor types; however, Fotivda’s potency, selectivity, and long half-life are hypothesized to improve the drug’s efficacy and safety in comparison to its predecessors.
Cancer cells are known to rely on glycolysis as an energy source. CB-839 (Calithera Biosciences) inhibits the glutaminase enzyme, reducing the ability of cancer cells to utilize glutamine in this biochemical pathway, thereby reducing cell proliferation and tumor growth.
Abexinostat (Xynomic Pharmaceuticals) is a broad histone deacetylase (HDAC) inhibitor. HDAC enzymes (also known as lysine deacetylase) cleave acetyl groups from N-acetyl lysine amino acids on a histone.
Calquence (acalabrutinib; AstraZeneca/Acerta) is a novel, orally available, second-generation Bruton’s tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Inhibition of the BTK protein prevents the activation of the B-cell antigen receptor signaling pathway, which blocks both B-cell activation and BTK-mediated activation of downstream survival pathways.
Copiktra (duvelisib; Verastem/Yakult Honsha) is a highly selective small molecule inhibitor of the p110-delta and p110-gamma isoforms of the phosphoinositide 3-kinase (PI3K) enzyme.
Zanubrutinib (BeiGene) is an oral small molecule inhibitor of Bruton’s tyrosine kinase (BTK), developed to be more selective with less off-target effects than Imbruvica (ibrutinib; AbbVie/Johnson & Johnson). BTK is part of the B-cell receptor signaling pathway, which promotes cell proliferation, adhesion, and survival in many B-cell malignancies.
INCB050465 (Incyte) is an oral phosphoinositide 3-kinase (PI3K) delta-specific inhibitor. The PI3K pathway has been shown to be highly active in a subset of follicular lymphoma (FL), promoting cell proliferation and survival. INCB050465 inhibits the PI3K-delta isoform with a 20,000-fold selectivity over other PI3K isoforms.
Betalutin is a first-in-class antibody-radionucleotide conjugate targeted to CD37, an alternative to CD20, which is widely targeted in non-Hodgkin’s lymphoma. CD37 is highly expressed in B cells and B-cell lymphomas.
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.
MT-2271 is a plant-based, recombinant virus-like particle (VLP) QIV seasonal influenza vaccine in development by Mitsubishi Tanabe Pharma. It contains a mix of recombinant hemagglutinin proteins expressed as VLPs.
Flublok (Sanofi) is a quadrivalent recombinant seasonal influenza vaccine that contains antigens from two A strains and two B strains specified by the World Health Organization seasonally for influenza vaccination.
Fluzone HD (inactivated split virion; Sanofi Pasteur) is an inactivated influenza vaccine that contains antigens from two A strains and one B strain specified by the World Health Organization seasonally for influenza vaccination.
Flucelvax is an inactivated subunit cell-based QIV that contains antigens from two A strains and two B strains specified by the World Health Organization seasonally for influenza vaccination.
FluMist QIV (AstraZeneca/Daiichi Sankyo) is a quadrivalent live-attenuated influenza vaccine containing antigens from two A strains and two B strains specified by the World Health Organization seasonally for influenza vaccination.
Fluad QIV (CSL) is a subunit, surface antigen-containing seasonal quadrivalent influenza vaccine adjuvanted with MF-59, an oil-in-water emulsion. It contains antigens from two A strains and two B strains specified by the World Health Organization seasonally for influenza vaccination.
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.
Ralinepag (Arena Pharmaceuticals/Everest Medicines) is a selective prostaglandin I2 receptor agonist. PGI2 agonists are potent vasodilators and platelet aggregation inhibitors, which also help relax smooth muscle cells by counteracting the effect of vasoconstrictive mediators.
Esuberaprost (United Therapeutics) is an oral chemically stable prostacyclin analog targeting the prostaglandin I2 (PGI2) receptor. PGI2 agonists are potent vasodilators and platelet aggregation inhibitors, and also help relax smooth muscle cells by counteracting the effect of vasoconstrictive mediators.
Bardoxolone methyl (AbbVie/Kyowa Hakko Kirin), under development by the research-stage company Reata Pharmaceuticals, is a Phase III candidate in clinical trials for the treatment of pulmonary arterial hypertension.
INOpulse (Bellerophon Therapeutics) is a drug-device combination being developed to deliver a continuous, pulsed dose of nitric oxide via intranasal inhalation.
United Therapeutics is developing a gene therapy product called Aurora-GT (endothelial nitric oxide-synthase-enhanced endothelial progenitor cells)
United Therapeutics developed Tyvaso (treprostinil) as a follow-on product to Remodulin. As an inhaled formulation of treprostinil
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).
Lisocabtagene maraleucel (also known as JCAR017; Celgene) will be the third autologous chimeric antigen receptor T-cell (CAR-T) therapy to reach the diffuse large B-cell lymphoma (DLBCL) market following the launches of approved CAR-T drugs Kymriah (tisagenlecleucel; Novartis) and Yescarta (axicabtagene ciloleucel; Gilead).
Polatuzumab vedotin (Roche) is an antibody-drug conjugate (ADC) that combines a humanized immunoglobulin (Ig)-G1 monoclonal antibody (MAb) targeting human B-cell surface antigen cluster of differentiation (CD)79b and antimitotic agent monomethyl auristatin E (MMAE).
MorphoSys is positioning its cluster of differentiation (CD)19-targeted monoclonal antibody MOR208 in relapsed/refractory diffuse large B-cell lymphoma (DLBCL) patients who are ineligible for high-dose chemotherapy and autologous stem cell transplant.
Umbralisib (TG Therapeutics/Rhizen) is a novel phosphoinositide 3-kinase (PI3K) delta inhibitor that also selectively inhibits casein kinase-1 (CK1) epsilon. Expression of the PI3K delta isoform plays a role in B-cell development and function, and is often overactivated in B-cell malignancies.
Kinenza (enzastaurin) is an oral serine/threonine kinase inhibitor that suppresses signaling of protein kinase C (PKC)-beta to induce cell apoptosis, reduce cell proliferation, and suppress tumor-induced angiogenesis.
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