Rivaroxaban
- Generic Name
- Rivaroxaban
- Brand Names
- Xarelto, Rivaroxaban Accord, Rivaroxaban Viatris (previously Rivaroxaban Mylan)
- Drug Type
- Small Molecule
- Chemical Formula
- C19H18ClN3O5S
- CAS Number
- 366789-02-8
- Unique Ingredient Identifier
- 9NDF7JZ4M3
- Background
Rivaroxaban is an anticoagulant and the first orally active direct factor Xa inhibitor. Unlike warfarin, routine lab monitoring of INR is not necessary. However there is no antidote available in the event of a major bleed. Only the 10 mg tablet can be taken without regard to food. The 15 mg and 20 mg tablet should be taken with food. FDA approved on July 1, 2011.
- Indication
Rivaroxaban is indicated for the prevention of venous thromboembolic events (VTE) in patients who have undergone total hips replacements and total knee replacement surgery; prevention of stroke and systemic embolism in patients with nonvalvular atrial fibrillation; treatment of deep vein thrombosis (DVT) and pulmonary embolism (PE); to reduce risk of recurrent DVT and/or PE. Rivaroxaban is also indicated, in combination with aspirin, for reducing the risk of major cardiovascular events in patients with chronic coronary artery disease or peripheral artery disease. Its use is also not recommended in those with severe renal impairment (<30mL/min).
Rivaroxaban is also indicated for the treatment and prevention of VTE in pediatric patients (from birth to 18 years of age) and for thromboprophylaxis in pediatric patients ≥2 years old with congenital heart disease following the Fontan procedure.
- Associated Conditions
- Cardiovascular Mortality, Deep Vein Thrombosis, Deep vein thrombosis recurrent, Major Adverse Cardiovascular Events, Myocardial Infarction, Pulmonary Embolism, Recurrent Pulmonary Embolism (Disorder), Recurrent Venous Thromboembolism, Stroke, Systemic Embolism, Thrombosis, Venous Thromboembolism
Lupin Receives FDA Approval for Generic Rivaroxaban Tablets for Thrombosis Prevention
• Lupin has received U.S. FDA approval for its generic version of Rivaroxaban Tablets, expanding its cardiovascular portfolio with a key anticoagulant medication.
• Rivaroxaban is primarily indicated for the prevention and treatment of deep vein thrombosis, pulmonary embolism, and stroke prevention in patients with atrial fibrillation.
• The approval represents a significant milestone for Lupin in the competitive generic pharmaceutical market, potentially offering a more affordable alternative to Janssen's branded Xarelto.
2025 Pharmaceutical Pipeline: Major Patent Expirations Set to Transform Drug Market with Generics and Biosimilars
• The US pharmaceutical market is poised for significant change in 2025 as several blockbuster drugs including Xarelto, Entresto, and Stelara face patent expirations, opening the door to generic and biosimilar competition.
• Multiple biosimilars for ustekinumab (Stelara) are entering the market in 2025, with Wezlana already launched in January as the first interchangeable biosimilar, while other major drugs like ticagrelor and denosumab will also face competition.
• The pharmaceutical pipeline continues to expand with innovative therapies for cancer and neurological disorders, alongside the Medicare Drug Price Negotiation program which will further impact pricing dynamics for high-cost medications.
Vividion Therapeutics Initiates Phase I Trial of Novel RAS-PI3Kα Inhibitor for Advanced Solid Tumors
• Vividion Therapeutics has dosed the first patient in a Phase I trial of VVD-159642, an oral inhibitor targeting the RAS-PI3Kα pathway implicated in approximately 20% of all cancers.
• The study will evaluate VVD-159642 as both monotherapy and in combination with sotorasib or trametinib in patients with advanced solid tumors, potentially offering a new treatment approach for RAS-driven cancers.
• VVD-159642 represents Vividion's fourth clinical-stage program from its chemoproteomics platform, designed to selectively inhibit oncogenic signaling while avoiding toxicities that have limited previous attempts to target this pathway.
Low-Dose Apixaban Proves Effective and Safer for Extended Cancer-Related VTE Prevention
• The API-CAT trial demonstrated that reduced-dose apixaban (2.5mg twice daily) was noninferior to full-dose (5mg twice daily) for preventing recurrent venous thromboembolism in cancer patients requiring extended anticoagulation.
• Patients receiving the lower dose experienced significantly fewer bleeding events (12.1% vs 15.6%) while maintaining similar protection against blood clots, potentially changing clinical practice guidelines for cancer-associated thrombosis management.
• The findings are particularly significant as cancer patients live longer with improved treatments but face ongoing thrombosis risks, offering clinicians a safer option for long-term anticoagulation beyond the initial 6-month treatment period.
Biocon Pharma Secures FDA Approval for Norepinephrine Bitartrate Injection for Acute Hypotension
• Biocon Pharma Limited, a wholly owned subsidiary of Biocon Limited, has received FDA approval for Norepinephrine Bitartrate Injection USP, used to raise blood pressure in adults with acute hypotension.
• The approved product is packaged as a 4 mg/4 mL (1 mg/mL) single-dose vial and serves as a critical treatment in emergency medical and intensive care settings.
• This approval strengthens Biocon's growing portfolio of complex drug products and expands its presence in the U.S. pharmaceutical market, particularly in the complex injectables segment.
FDA Grants Fast Track Designation for Johnson & Johnson's Nipocalimab in Sjögren's Disease
• The FDA has granted Fast Track Designation for Johnson & Johnson's nipocalimab to treat Sjögren's disease, following its earlier Breakthrough Therapy Designation, potentially accelerating development for this autoimmune condition.
• Johnson & Johnson reported an 11% share price increase over the last quarter, bolstered by multiple regulatory milestones including Health Canada's approval for LAZCLUZE and positive results from the ANTHEM-UC study for ulcerative colitis.
• Despite broader market volatility and a one-off $7.8 billion loss impacting recent financial results, J&J has maintained investor confidence through consistent dividend increases and strategic focus on its pharmaceutical portfolio.
Lupin Launches First Generic Xarelto in US Market Despite Ongoing Patent Litigation
• Lupin has begun rolling out the first generic version of the blockbuster anticoagulant Xarelto (rivaroxaban) in the US market after the Patent Trial and Appeal Board invalidated a key patent.
• The FDA has approved generic Xarelto applications from both Lupin and Sun Pharma's Taro subsidiary, marking significant competition for the J&J/Bayer blockbuster that generates billions in annual revenue.
• Despite the launch, both generic manufacturers remain entangled in litigation with J&J/Bayer over a patent that doesn't expire until 2039, creating uncertainty about potential damages if the patent is ultimately upheld.
Lupin Launches Generic Rivaroxaban in US Market Following FDA Approval
• Lupin has launched Rivaroxaban Tablets USP, 2.5 mg in the US market after receiving final approval from the FDA for its Abbreviated New Drug Application.
• The generic equivalent of Janssen's Xarelto® targets patients with coronary artery disease and peripheral artery disease, with estimated annual US sales of $446 million.
• This strategic launch strengthens Lupin's position in the high-value anticoagulant market, following the company's strong Q3 performance with a 38.8% increase in profit.
Pharmaceutical Industry Braces for $236 Billion Patent Cliff by 2030: Strategic Responses from Major Players
• The global pharmaceutical industry faces a $236 billion patent cliff between 2025-2030, with nearly 70 blockbuster drugs losing exclusivity and exposing major companies to significant revenue losses.
• Key drugs approaching patent expiration include Merck's Keytruda ($25B), Bristol-Myers Squibb's Eliquis ($12B), and Johnson & Johnson's Stelara ($10.9B), forcing companies to rapidly adapt through pipeline diversification and cost-cutting measures.
• Companies are responding with increased M&A activity, AI-driven R&D efficiency, and strategic pivots to high-growth therapeutic areas, while the cliff will likely improve drug affordability but potentially slow innovation.
Biocon Pharma Secures FDA Approval for Generic Cancer and Blood Disorder Treatments
• Biocon Pharma Limited has received FDA approval for generic Lenalidomide capsules in six strengths, expanding treatment options for multiple myeloma and other blood disorders.
• The company gained approval for Dasatinib tablets in six different strengths, providing an alternative therapy for chronic myeloid leukemia and acute lymphoblastic leukemia patients.
• A tentative approval for Rivaroxaban tablets was also secured, positioning Biocon to offer treatment options for deep vein thrombosis and stroke prevention in atrial fibrillation patients.
FDA Approves First Generic Rivaroxaban 2.5mg for Cardiovascular and Peripheral Artery Disease Prevention
• The FDA has approved the first generic version of Xarelto (rivaroxaban) 2.5mg tablets for reducing major cardiovascular events in coronary artery disease patients and thrombotic events in peripheral artery disease patients.
• The approval marks a significant milestone in expanding access to anticoagulant medications, as blood thinners are among the most frequently prescribed drugs in the United States.
• This generic approval aligns with FDA's commitment to providing more affordable treatment options while maintaining safety and efficacy standards for cardiovascular disease management.
FDA Approves Genentech's TNKase for Acute Ischemic Stroke with Simplified Administration
• The FDA has approved Genentech's TNKase, a clot-dissolving agent, for treating acute ischemic stroke in adults, marking the company's second stroke treatment approval.
• TNKase offers a streamlined five-second intravenous bolus administration, presenting a significant advantage over the current standard treatment Activase's 60-minute infusion protocol.
• The approval is supported by a multi-center non-inferiority study across 22 Canadian stroke centers, demonstrating comparable safety and efficacy to Activase in patients with disabling neurological deficits.
Novartis Acquires Anthos Therapeutics for $925M, Aims to Advance Novel Blood Thinner Abelacimab
• Novartis has announced a $3 billion deal to acquire Anthos Therapeutics, securing rights to abelacimab, a Factor XI inhibitor blood thinner designed to be safer than existing anticoagulants.
• The acquisition includes a $925 million upfront payment and potential milestone payments of up to $2.15 billion, with the deal expected to close in first half of 2025.
• Recent Phase 2 trial results showed abelacimab demonstrated superior safety compared to Xarelto, with three Phase 3 trials currently ongoing in patients with atrial fibrillation and cancer-associated blood clotting.
Novartis to Acquire Anthos Therapeutics for $925M, Advancing Novel Stroke Prevention Drug Abelacimab
• Novartis has entered into an agreement to acquire Anthos Therapeutics for $925 million upfront, with potential additional payments of up to $2.15 billion based on milestone achievements.
• Abelacimab, a first-in-class Factor XI inhibitor antibody, demonstrated significant reduction in bleeding events compared to standard anticoagulants in Phase 2 trials for atrial fibrillation patients.
• The acquisition strengthens Novartis's cardiovascular portfolio with a late-stage asset that has received FDA Fast Track Designation for both cancer-associated thrombosis and stroke prevention in atrial fibrillation.
Bayer Advances Asundexian to Phase 3 Despite Phase 2 Efficacy Misses
• Bayer is proceeding with Phase 3 trials for asundexian, an oral Factor XIa inhibitor, despite it failing to meet primary efficacy endpoints in Phase 2 studies for ischemic stroke and acute myocardial infarction.
• The OCEANIC trial program will assess asundexian in up to 30,000 patients with atrial fibrillation, non-cardioembolic ischemic stroke, or high-risk transient ischemic attack.
• Phase 2 PACIFIC studies showed asundexian's safety profile was comparable to placebo, without increased bleeding, supporting its continued development despite the lack of efficacy.
• Bristol-Myers Squibb and Johnson & Johnson are also developing a Factor XIa inhibitor, milvexian, which showed promising results in secondary stroke prevention, intensifying competition in this drug class.
Pharma Stock Roundup: Novo Nordisk's Obesity Study Disappoints, Lilly's Zepbound Approved for Sleep Apnea
• Novo Nordisk's CagriSema obesity treatment showed a 22.7% weight loss in Phase III, falling short of the anticipated 25% reduction, impacting stock prices.
• Eli Lilly's Zepbound (tirzepatide) received FDA approval for moderate-to-severe obstructive sleep apnea (OSA), marking it as the first drug for obesity-related OSA.
• AstraZeneca and Daiichi Sankyo withdrew their EU application for Dato-DXd in non-small cell lung cancer (NSCLC) but pursue U.S. approval for EGFR-mutated NSCLC.
• Pfizer's Braftovi gained FDA approval in combination with Erbitux and mFOLFOX6 for first-line treatment of metastatic colorectal cancer with BRAF mutations.
Nuvation Bio's Taletrectinib Gains FDA Priority Review and Expanded Access Program for ROS1+ NSCLC
• The FDA granted priority review to Nuvation Bio's NDA for taletrectinib, a next-generation ROS1 inhibitor, for advanced ROS1+ non-small cell lung cancer, setting a PDUFA date of June 23, 2025.
• Taletrectinib demonstrated promising efficacy and tolerability in the TRUST-I and TRUST-II trials, showing durable responses and prolonged progression-free survival in ROS1+ NSCLC patients.
• Nuvation Bio has initiated an Expanded Access Program (EAP) in the U.S. for taletrectinib, offering access to eligible patients with advanced ROS1+ NSCLC outside of clinical trials.
• The NDA is based on pooled data from the TRUST-I and TRUST-II studies, which included over 300 patients, representing the largest ROS1-positive NSCLC dataset supporting an NDA.
Eli Lilly's Zepbound Demonstrates Superior Weight Loss Compared to Novo Nordisk's Wegovy in Head-to-Head Trial
• Eli Lilly's Zepbound (tirzepatide) led to a 20.2% average weight loss, significantly outperforming Wegovy (semaglutide) at 13.7% in a 72-week clinical trial.
• The SURMOUNT-5 trial included overweight or obese adults without diabetes, showing Zepbound users experienced 47% more relative weight loss than Wegovy users.
• Zepbound, a dual GIP and GLP-1 receptor agonist, helped 31.6% of participants achieve at least 25% body weight loss, compared to 16.1% with Wegovy.
• The study's findings may influence treatment choices, with Zepbound potentially becoming a preferred option for greater weight loss outcomes, pending further data on tolerability.
Acoramidis Gains Global Momentum: FDA Approval, EU Recommendation, and Promising Clinical Data
• Acoramidis (Attruby), developed by Stanford Medicine and BridgeBio, receives FDA approval for transthyretin amyloid cardiomyopathy (ATTR-CM) treatment, marking a significant milestone.
• The European Medicines Agency's CHMP recommends acoramidis for EU marketing authorization based on positive Phase 3 ATTRibute-CM trial results.
• Clinical trials demonstrate acoramidis' efficacy in reducing cardiovascular-related hospitalizations and improving survival rates for ATTR-CM patients.
• Bayer and BridgeBio collaborate to commercialize acoramidis, with Bayer holding EU rights and plans for a launch in Europe in early 2025.
Abelacimab Shows Promise in Reducing Bleeding Risk for Atrial Fibrillation Patients
• The AZALEA-TIMI 71 trial demonstrated that abelacimab significantly reduces bleeding events compared to rivaroxaban in atrial fibrillation patients.
• Abelacimab, a Factor XI inhibitor, showed a 62% to 69% reduction in major or clinically relevant non-major bleeding compared to rivaroxaban.
• Gastrointestinal bleeding, a common issue with current anticoagulants, was almost eliminated with abelacimab treatment.
• A Phase III trial (LILAC-TIMI 76) is underway to assess abelacimab's efficacy in preventing stroke in high-risk patients ineligible for current anticoagulants.
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