Tafluprost

This article will review currently applied listed GPCR-targeting drugs, and the associated popular GPCR class targets and drug development opportunities worth paying attention to. 1.Eli Lilly: TirzepatideTarget:GIPR + GLP-1R Tirzepatide is a novel GIPR and GLP-1R dual agonist developed by Eli Lilly. In preclinical and clinical trials, compared to selective GLP-1 receptor agonists, GIP/GLP-1 dual agonists have been shown to better control blood sugar and reduce weight. Therefore, it is receiving increasing attention as a new therapeutic drug for controlling blood sugar and weight. In 2022, Tirzepatide was approved for the first time in the United States for the treatment of adult type II diabetes as an adjunct to diet and exercise. Subsequently, Tirzepatide was approved in the European Union and Japan for the treatment of type II diabetes. 👇Please click on the image below to directly access the latest data (R&D Status | Core Patent | Clinical Trial | Approval status in Global countries) of this drug. 2.ChemoCentryx: AvacopanTarget:C5aR Avacopan(Tavneos) is an orally administered, first-in-class selective complement 5a receptor (C5aR) antagonist, discovered and developed by ChemoCentryx. This drug is used as an adjunctive therapy for ANCA-associated vasculitis in adult patients. Anti-neutrophil cytoplasmic antibody-associated vasculitis (AAV) is a rare ("oligo-immune") systemic small-vessel vasculitis, with an estimated incidence of 3 per 100,000 annually, characterized by the presence of ANCAs in the serum. The entire course of AAV includes granulomatosis with polyangiitis (GPA), microscopic polyangiitis (MPA), eosinophilic granulomatosis with polyangiitis (EGPA), and drug-induced AAV. Despite its complex pathophysiology, research over the past approx. 20 years has determined the crucial role of the alternative complement pathway, particularly the interaction of C5a with the C5aR receptor in AAV. Avacopan was first approved for marketing in Japan on September 27, 2021, and was subsequently approved in the United States, European Union, Canada, and Australia for the treatment of adult patients with ANCA-associated vasculitis, granulomatosis with polyangiitis, and microscopic polyangiitis. In addition, research is ongoing for other potential clinical indications, such as hidradenitis suppurativa and C3 glomerulopathy. 3.Pfizer: Rimegepant Sulfate Target:CGRP Receptor Rimegepant is an orally administered CGRP receptor antagonist used for the acute treatment of migraine in adults, with or without aura.  Initially developed by the BMS(BMS-742413), the newly established biotech company Biohaven Pharmaceutical acquired the exclusive global development and commercialization rights to Rimegepant in 2016. The Biohaven team conducted a series of clinical studies and analyses around Rimegepant and developed the derivative migraine nasal spray drug, Zavegepant.  In May 2022, Pfizer announced that it would acquire Biohaven for a total cash consideration of approximately 11.6 billion USD. Rimegepant was first approved for marketing in the United States on February 27, 2020, and subsequently received approval in Israel, the United Arab Emirates, Kuwait, the European Union, and Iceland, among others. Currently, the drug is being tested in clinical trials for conditions like chronic sinusitis, nasal polyps, and trigeminal neuralgia. 4. Glenmark:RYALTRISTarget:H1R+GR RYALTRIS is a new compound prescription nasal spray developed by the Indian pharmaceutical company, Glenmark. This medication has the dual efficacy of activating glucocorticoid receptor (GR) and antagonizing histamine H1 receptor (H1R). Mometasone is a moderately potent synthetic corticosteroid that acts as a glucocorticoid receptor agonist, possessing anti-inflammatory, anti-itch, and vasoconstrictive properties. Olopatadine, on the other hand, is an antagonist of histamine H1 receptors used for the treatment of allergic conjunctivitis and rhinitis. Since histamine is the primary inflammatory mediator causing inflammation and allergic reactions, Olopatadine works by blocking the action of histamine receptors. Compared to other anti-allergic ophthalmic drugs, Olopatadine does not interfere with the cell membrane, thus offering good comfort and tolerability. RYALTRIS was first approved for marketing in Australia in 2019, and subsequently received approval for listing in South Africa, the UK, the US, Canada, and other countries.  In 2019, Grand Pharmaceutical and Glenmark signed an exclusive licensing agreement, in which Glenmark granted Grand Pharmaceutical the exclusive rights to sell RYALTRIS in China. Glenmark would be responsible for the manufacture and supply of the authorized product, while Grand Pharmaceutical would be in charge of the clinical trials and registration work for the authorized product in China and can exclusively sell the approved product in China for 20 years upon approval. 5. Amgen:ErenumabTarget:CGRP Erenumab is a human monoclonal antibody developed by Amgen and is the first monoclonal antibody drug targeting GPCR approved by the FDA. Erenumab can specifically bind to and antagonize the Calcitonin Gene-Related Peptide Receptor (CGRPR), thus preventing migraines. In April 2017, Amgen announced an expanded commercial collaboration with Novartis on Erenumab, which is being studied for the prevention of migraine. This expanded business cooperation is based on the global neuroscience collaboration established by Novartis and Amgen in 2015 in the areas of Alzheimer's disease and migraine.  Novartis initiated two clinical trials in China in 2019 to evaluate the safety and efficacy of Erenumab injection in the treatment of migraines.  Erenumab was first approved for marketing in the United States in 2018, and was subsequently approved in Australia, Iceland, Norway, Switzerland, Canada, and Japan.  In addition to the treatment of migraines, clinical trial research is ongoing for other indications, including headaches, hot flashes, temporomandibular joint dysfunction syndrome, stable angina. 6. Kyowa Kirin:EvocalcetTarget:CaSR Evocalcet is a Calcium-Sensing Receptor (CaSR) agonist developed by Kyowa Kirin, used for the treatment of hypercalcemia, secondary hyperparathyroidism, and other related conditions.  Kyowa Kirin has applied for two clinical trials in China to evaluate the effectiveness of Evocalcet in treating secondary hyperparathyroidism in patients undergoing maintenance dialysis for chronic kidney disease.  As of now, Evocalcet has only been approved for marketing in Japan. 7. Otsuka Pharmaceutical: BrexpiprazoleTarget:5-HT1A+5-HT2A+D2R Brexpiprazole is a serotonin-dopamine activity modulator developed by Otsuka Pharmaceutical, used as an adjunctive treatment for severe depression, schizophrenia, and agitation associated with dementia caused by Alzheimer's disease. Brexpiprazole is an atypical antipsychotic and a novel D2 dopamine and serotonin 1A partial agonist, known as a serotonin-dopamine activity modulator. It has a high affinity for serotonin, dopamine, and alpha-adrenergic receptors. Structurally, Brexpiprazole is very similar to another atypical antipsychotic drug, Aripiprazole, but Brexpiprazole has a different affinity for binding with dopamine and serotonin receptors. Compared to Aripiprazole, Brexpiprazole is less likely to produce adverse reactions mediated by partial agonist, such as extrapyramidal symptoms, due to its lower intrinsic activity at the D2 receptor. Brexpiprazole was first approved in the United States in 2015, and subsequently approved in Canada, Japan, and the European Union. In addition to treating depression, this drug is undergoing global clinical trials and research for multiple indications including agitation, schizophrenia, Alzheimer's disease, and performance anxiety. 8. Santen: TapcomTarget:PTGFR+βAR Tapcom is a combination eye drop medication containing Tafluprost and Timolol Maleate, developed by Santen. Tafluprost is a prostaglandin analogue used in ophthalmology to reduce intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Chemically, Tafluprost is a fluorinated analogue of prostaglandin F2-α. Timolol is a non-selective beta-adrenergic antagonist, used for the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.  Tapcom was first approved for marketing in Japan in 2013, and subsequently received approval in countries including Iceland, France, Poland, and Germany. 9. Takeda:TeduglutideTarget:GLP-2R Teduglutide is a glucagon-like peptide-2 (GLP-2) analog developed by the British rare disease pharmaceutical giant, Shire Development, for the treatment of patients with short bowel syndrome (SBS) who require parenteral nutrition support. Teduglutide is comprised of 33 amino acids, and is manufactured using strains of E. coli that have been modified through DNA recombinant technology. Teduglutide differs from GLP-2 by one amino acid (alanine is replaced with glycine). This substitution results in Teduglutide having a longer duration of action than endogenous GLP-2 and a higher resistance to hydrolysis by the enzyme dipeptidyl peptidase-4.  Teduglutide first received regulatory approval within the European Union in 2012, followed by approval in the United States and Japan, in all cases for the treatment of SBS.  In 2019, Takeda Pharmaceuticals spent an astounding £46 billion to acquire Shire Development, in a move that has been dubbed as a "snake swallowing an elephant" merger in the pharmaceutical world. This acquisition propelled Takeda Pharmaceuticals into the list of top 10 global biopharmaceutical companies. Clinical research on the application of Teduglutide for the treatment of Crohn's Disease and kidney disorders was discontinued due to this acquisition. 10. AstraZeneca: Duaklir GenuairTarget:M3R+β2AR Duaklir Genuair is a combined Aclidinium Bromide/Formoterol Fumarate inhalation powder developed by AstraZeneca. This medication is used as a maintenance bronchodilator to alleviate the symptoms of disease in adults with chronic obstructive pulmonary disease (COPD). Among them, Aclidinium bromide is a novel long-acting muscarinic antagonist, and Formoterol fumarate is a long-acting β2 receptor agonist.  Duaklir Genuair is administered by the Genuair dry powder inhaler twice a day and is the first combined medication that has shown a statistically significant improvement over monotherapy in terms of shortness of breath. Duaklir Genuair was first approved in the European Union in 2012, and subsequently in the United States in 2019, for the treatment of chronic obstructive pulmonary disease.

IYUZEH™ (latanoprost ophthalmic solution) 0.005%, the first and only preservative-free formulation of latanoprost, the most prescribed prostaglandin F2α analogue (PGA), is now available in the U.S. WALTHAM, Mass., Sept. 26, 2023 /PRNewswire/ -- Thea Pharma Inc. ("Thea"), the U.S. subsidiary of Europe's leading independent ophthalmic-focused pharmaceutical company, Théa, dedicated to the research, development, and commercialization of ophthalmic products, today announced the launch and availability of IYUZEH™ (latanoprost ophthalmic solution) 0.005% in the U.S. market. Preservative-free latanoprost, launched over ten years ago, is available in 46 countries, mostly under the brand name MONOPROST®, with about 1.5 million patients treated monthly.1 IYUZEH is the first and only preservative-free latanoprost for patients with primary open-angle glaucoma (POAG) and ocular hypertension (OHT) in the U.S. In randomized, controlled clinical trials of patients with POAG or OHT with mean baseline intraocular pressure (IOP) of 19-24 mmHg, IYUZEH lowered IOP by 3–8 mmHg compared to 4–8 mmHg by XALATAN®.2-4 Experience the full interactive Multichannel News Release here: "The U.S. launch of IYUZEH is a major step forward for Théa Group, the eye care community, and patients," said Jean-Frédéric Chibret, President of Théa. "Glaucoma is a chronic eye disease that affects the everyday lives of more than 60 million people globally. With IYUZEH now available, eye care providers can effectively treat their POAG and OHT patients with preservative-free latanoprost. I would like to thank everyone involved in achieving this milestone – including the providers and patients who participated in the clinical studies, our teams, and each of our partners – for helping us deliver on our commitment to enable patients access to medication without preservatives." "With the launch of IYUZEH in the U.S., Thea is responding to an important unmet need in the treatment landscape. IYUZEH brings similar efficacy of traditional latanoprost, formulated without preservatives, to help eye care providers confidently address their treatment goals of lowering intraocular pressure for people with POAG and OHT," said Susan Benton, President of Thea Pharma Inc. "We are thrilled to introduce IYUZEH and provide clinicians with an important new treatment option for their patients." "With the availability and proven efficacy of IYUZEH, it is now possible for eye care providers to lower elevated intraocular pressure in patients with POAG or OHT without preservatives on the ocular surface," said Jason Bacharach, M.D., Founder and Director of Research at North Bay Eye Associates in Petaluma, California. "This is a powerful option for our patients and for us, as treating clinicians." IYUZEH is available now through authorized distributors and the following wholesalers and order numbers: ABC (10282592), ANDA (603442), Cardinal (5865035), McKesson (2849651), NDC (82584-003-30). From enrollment to dispensing, Thea is committed to supporting eye care professionals and patients in every step of the access process. IYUZEH (latanoprost ophthalmic solution) 0.005% is now available for as little as $60 for a 30-day supply through programs with PhilRx® and the Thea Savings Card. For more information and eligibility requirements, please visit iyuzeh.com. PhilRx is a service that provides a convenient way to prescribe IYUZEH, with the medication shipped for free and directly to a patient's door. This service offers online and phone support for both eye care professionals and their patients. The Thea Savings Card is available to those commercially insured and not enrolled in a state or federally funded program. A patient may check their eligibility and activate this savings card at activatethecard.com/theasavingscard. Whether a physical or digital card, it can be utilized or redeemed at any retail pharmacy in the U.S. Thea is committed to helping patients have access to IYUZEH. A Patient Assistance Program is available for eligible U.S. patients that have a demonstrated financial need and are without prescription insurance coverage. With this program, we aim to allow every qualified patient the chance to see their treatment with eyes wide open. About IYUZEH™ IYUZEH™ (latanoprost ophthalmic solution) 0.005%, an opalescent, white to slightly yellow ophthalmic solution, is a topical formulation of latanoprost that is indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma (OAG) or ocular hypertension (OHT). IYUZEH™ does not contain a preservative – it is the first and only preservative-free formulation of latanoprost, the most prescribed prostaglandin F2α analogue (PGA), in the United States. The recommended dosage of IYUZEH™ is one drop in the affected eye(s) once daily in the evening. If one dose is missed, treatment should continue with the next dose as normal. Reduction of the IOP starts approximately 3 to 4 hours after administration and the maximum effect is reached after 8 to 12 hours. IOP reduction is present for at least 24 hours. In the two clinical trials conducted with IYUZEH™ (latanoprost ophthalmic solution) 0.005%, the most frequently reported ocular adverse reactions were conjunctival hyperemia (34%) and eye irritation (19%) compared to XALATAN®, the preserved 0.005% latanoprost reference product which reported conjunctival hyperemia (37%) and eye irritation (31%). Healthcare providers, patients, and caregivers can learn more about IYUZEH at iyuzeh.com. INDICATIONS AND USAGE IYUZEH is a prostaglandin F2α analogue indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. IMPORTANT SAFETY INFORMATION CONTRAINDICATIONS Known hypersensitivity to latanoprost or any other ingredients in this product. WARNINGS AND PRECAUTIONS Pigmentation: Topical latanoprost ophthalmic products, including IYUZEH™ have been reported to cause changes to pigmented tissues. The most frequently reported changes have been increased pigmentation of the iris, periorbital tissue (eyelid), and eyelashes. Pigmentation is expected to increase as long as latanoprost is administered. The pigmentation change is due to increased melanin content in the melanocytes rather than to an increase in the number of melanocytes. After discontinuation of latanoprost, pigmentation of the iris is likely to be permanent, while pigmentation of the periorbital tissue and eyelash changes have been reported to be reversible in some patients. Patients who receive treatment should be informed of the possibility of increased pigmentation. The long-term effects of increased pigmentation are not known. Iris color change may not be noticeable for several months to years. Typically, the brown pigmentation around the pupil spreads concentrically towards the periphery of the iris and the entire iris or parts of the iris become more brownish. Neither nevi nor freckles of the iris appear to be affected by treatment. While treatment with IYUZEH™ can be continued in patients who develop noticeably increased iris pigmentation, these patients should be examined regularly. Eyelash Changes: Latanoprost ophthalmic products, including IYUZEH™ may gradually change eyelashes and vellus hair in the treated eye; these changes include increased length, thickness, pigmentation, the number of lashes or hairs, and misdirected growth of eyelashes. Eyelash changes are usually reversible upon discontinuation of treatment. Intraocular Inflammation: IYUZEH™ should be used with caution in patients with a history of intraocular inflammation (iritis/uveitis) and should generally not be used in patients with active intraocular inflammation because inflammation may be exacerbated. Macular Edema: Macular edema, including cystoid macular edema, has been reported during treatment with latanoprost ophthalmic products, including IYUZEH™. IYUZEH™ should be used with caution in aphakic patients, in pseudophakic patients with a torn posterior lens capsule, or in patients with known risk factors for macular edema. Herpetic Keratitis: Reactivation of herpes simplex keratitis has been reported during treatment with latanoprost. IYUZEH™ should be used with caution in patients with a history of herpetic keratitis. IYUZEH™ should be avoided in cases of active herpes simplex keratitis because inflammation may be exacerbated. Contact Lens Use: Contact lenses should be removed prior to the administration of IYUZEH™ and may be reinserted 15 minutes after administration. ADVERSE REACTIONS The following adverse reactions have been reported with the use of topical latanoprost products: iris pigmentation changes, eyelid skin darkening, eyelash changes (increased length, thickness, pigmentation, and number of lashes), intraocular inflammation (iritis/uveitis), and macular edema, including cystoid macular edema. DRUG INTERACTIONS The combined use of two or more prostaglandins, or prostaglandin analogs including IYUZEH™ is not recommended. It has been shown that administration of these prostaglandin drug products more than once daily may decrease the IOP lowering effect or cause paradoxical elevations in IOP. For more information about IYUZEH™, please visit iyuzeh.com. For Full Prescribing Information, please visit . About Primary Open-angle Glaucoma The American Glaucoma Society states that glaucoma is a common ophthalmic disorder characterized by typical optic nerve damage and vision loss. It is most associated with elevated or dysregulated intraocular pressure, although there is evidence that other factors contribute to the disease.5 Glaucoma is a leading cause of irreversible blindness worldwide. Its prevalence in the U.S. is approximately 1,900 per 100,000 persons over age forty, and the condition is responsible for upwards of nine million clinic visits each year.6-8 In the U.S., where annual spending on optic nerve disorders is estimated at $5.8 billion annually,9 glaucoma is a significant public health concern. About Ocular Hypertension Mean IOP slowly rises with increasing age. Age older than 40 years is considered a risk factor for the development of OHT and POAG.10 OHT, a common condition, is a leading risk factor for the development of OAG.11 OHT is defined as IOP consistently greater than 21 mmHg (in at least one eye) and the absence of clinical signs of glaucoma.12 The risk of developing glaucoma increases with increasing IOP.13 Population studies such as the Framingham, Beaver Dam, Baltimore, Rotterdam, Barbados, and Egna-Neumarkt studies estimate that 4-10% of the population older than 40 years will have IOP levels of 21 mmHg or higher without detectable signs of glaucomatous damage. OHT has a 10-15 times greater prevalence than POAG.14 The use of topical IOP-lowering medications reduced the risk of glaucoma development from 9.5% in the control group to 4.4% in the intervention group.15 About Théa Laboratoires Théa is an independent pharmaceutical company specialized in the research, development, and commercialization of eye-care products. Based in Clermont-Ferrand, France, it has thirty-five affiliates & offices in Europe, North and South America, North Africa, and the Middle East. Today, its network includes nearly 1,900 employees, and its products are available in 75 countries around the world. In 2022, Théa had global revenues of approximately $941 million. The independent and family-owned and run group, founded from a Research and Development start-up by Henri Chibret, has been chaired since 2008 by Jean-Frédéric Chibret, his nephew. To learn more about Théa Group, visit . About Thea Pharma, Inc. Thea Pharma, Inc., is the United States subsidiary of Théa. Its product offering is comprised of a portfolio of seven leading eye-care products that are regulated or approved by the U.S. Food and Drug Administration (FDA), including Zioptan®, AcellFX™, Cosopt®, Cosopt® PF, Azasite®, Akten®, and Betimol®, iVIZIA™ dry-eye drops and eyelid hygiene products, and now IYUZEH™. By focusing our passion and expertise within the U.S. market, Thea Pharma's goal is to deliver uncompromising care that allows all stakeholders to envision the future of ophthalmic treatment with eyes wide open. To learn more about Thea Pharma, Inc., visit . References: Théa. Data on file. 2023. IYUZEH™ (latanoprost ophthalmic solution) 0.005%. Prescribing information. Thea Pharma Inc; 2022. Bacharach J, Ahmed IIK, Sharpe ED, Korenfeld MS, Zhang S, Baudouin C. Preservative-Free versus Benzalkonium Chloride–Preserved Latanoprost Ophthalmic Solution in Patients with Primary Open-Angle Glaucoma or Ocular Hypertension: A Phase 3 US Clinical Trial. Clin Ophthalmol. 2023;17:2575-2588. . Rouland JF, Traverso CE, Stalmans I, et al. Efficacy and safety of preservative-free latanoprost eyedrops, compared with BAK-preserved latanoprost in patients with ocular hypertension or glaucoma. Br J Ophthalmol. 2013;97(2):196–200. doi:10.1136/bjophthalmol-2012-302121. The American Glaucoma Society (AGS). Unmet needs in the detection, diagnosis, monitoring, treatment, and understanding of primary open angle glaucoma. 2021; 11. . Accessed March 1, 2023. Friedman DS, Wolfs RC, O'Colmain BJ, et al. Prevalence of open-angle glaucoma among adults in the United States. Arch Ophthalmol. 2004;122(4):532–538. doi:10.1001/archopht.122.4.532. Schappert SM. Office Visits for Glaucoma: United States, 1991-92. Vital and Health Statistics, Centers for Disease Control and Prevention / National Center for Health Statistics. 1995; March, No. 262. Lee PP, Walt JG, Doyle JJ, et al. A multicenter, retrospective pilot study of resource use and costs associated with severity of disease in glaucoma. Arch Ophthalmol. 2006;124(1):12–19. doi:10.1001/archopht.124.1.12. Wittenborn JS, Zhang X, Feagan CW, et al. The economic burden of vision loss and eye disorders among the United States population younger than 40 years. Ophthalmology. 2013;120(9):1728–35. . Leske MC, Connell AM, Wu SY, et al. Distribution of intraocular pressure. The Barbados Eye Study. Arch Ophthalmol. 1997 Aug. 115(8):1051-7. Kass MA, Heuer DK, Higginbotham EJ, et al. Assessment of Cumulative Incidence and Severity of Primary Open-Angle Glaucoma Among Participants in the Ocular Hypertension Treatment Study After 20 Years of Follow-up. JAMA Ophthalmol. 2021;139(5):558–566. doi:10.1001/jamaophthalmol.2021.0341. Burr JM, Botello-Pinzon P, Takwoingi Y, Hernandez R, Vazquez-Montes M, Elders A, et al. Surveillance for ocular hypertension: an evidence synthesis and economic evaluation. Health Technol Assess. 2012;16(29):1-271, iii-iv. Burr JM, Mowatt G, Hernandez R, Siddiqui MAR, Cook J, Lourenco T, et al. The clinical effectiveness and cost-effectiveness of screening for open angle glaucoma: a systematic review and economic evaluation. Health Technol Assess. 2007;11(41):iii-iv, ix-x, 1-190. Chihara E. Assessment of true intraocular pressure: the gap between theory and practical data. Surv Ophthalmol. 2008 May-Jun. 53(3):203-18. Kass MA, Heuer DK, Higginbotham EJ, et al. The Ocular Hypertension Treatment Study: A Randomized Trial Determines That Topical Ocular Hypotensive Medication Delays or Prevents the Onset of Primary Open-Angle Glaucoma. Arch Ophthalmol. 2002;120(6):701-713. doi:10.1001/archopht.120.6.701. PRC-IYZ-1676-v2 SOURCE Thea Pharma Inc.