Delving into the Latest Updates on Apixaban with Synapse

There are two parts of the study. In Part 1, the invesitgaotrs want to investigate whether treatment with apixaban improves pain and quality of life in patients with painful venous malformations The participants are randomized to different treatment orders of the two treatment periods with apixaban and placebo. Arm 1 starts apixaban followed by placebo and arm 2 starts with placebo followed by apixaban. Between the treatment sequences there will be a washout period of minimum one week.
The participants will register pain and use og pain medication in a diary every day for one week before start of treatment and before evaluation of effect. Also, a quality of life form will be filled out before each consultation.
In Part 2, the investigators will investigate long-term effect and safety of apixaban and reduce dose after 3 months to find the minimal effective dose.
Part 2 includes participants from Part 1 study who experienced effect of treatment or who agree to continue apixaban treatment. Study start of Part 2 is at the end of Part 1. All participants receive the same dose of apixaban as in part 1 (5 mg twice daily), and after 3 months (visit 2) the dose is reduced to 2.5 mg twice daily.

Start Date01 Feb 2025

Sponsor / Collaborator

Oslo universitetssykehus HF

TCTR20240715013 / Not yet recruitingPhase 1IIT

A Bioequivalence study of a randomized, open-label, single dose, two-way crossover design with two-period, two-treatment and two-sequence of Apixaban Tablet 5 mg, relative to EliquisTM, in healthy Thai volunteers under fasting condition

Start Date07 Jan 2025

Sponsor / Collaborator

Bio-innova Co., Ltd

100 Clinical Results associated with Apixaban

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100 Translational Medicine associated with Apixaban

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100 Patents (Medical) associated with Apixaban

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5,339

Literatures (Medical) associated with Apixaban

01 Jun 2025·Recent Patents on Nanotechnology

Formulation Optimization and Characterization of Solid Lipid Nanoparticles of Apixaban

Article

Author: Mulay, Laukik ; Hegde, Namita ; Kanugo, Abhishek

Background::

Unpredictable situations such as clotting of blood, deep vein thrombosis, and pulmonary embolism arise in the body, which is the leading cause of mortality. Such conditions generally arise after surgery as well as after treatment with oral anticoagulant agents. Apixaban is a novel oral anticoagulant widely recommended for the prevention and treatment of strokes and blood clots suffering from nonvalvular atrial fibrillation by suppressing factor Xa. Apixaban has a log P of 2.71 with poor solubility and reported maximum bioavailability of approximately 50%.

Objective::

Hence, the current research mainly focused on the improvement of solubility, bioavailability, and therapeutic efficacy of Apixaban via solid lipid nanoparticles (SLN).

Methods::

The SLN was developed using the hot-homogenization method using a high-pressure homogenizer. The drug-lipid compatibility study was assessed by the FTIR, and the thermal analysis was performed using differential scanning calorimetry (DSC). During the scrutiny of lipids, the highest solubility of Apixaban was estimated in the glyceryl monostearate, hence selected for the formulation. Moreover, the colloidal solution was stabilized by the polyethylene glycol 200. The Design of Expert software (Version 13, Stat-Ease) was implemented for the optimization analysis by considering the 3-independent factors and 2-dependent parameters. The Patents on the SLN are Indian 202321053691, U.S. Patent, 10,973,798B2, U.S. Patent, U.S. Patent 2021/0069121A1, U.S. Patent 2022/0151945A1.

Results::

Box-Behnken design was applied along with ANOVA, which showed a p-value less than 0.05 for the dependent parameters such as particle size and entrapment efficiency (p-value: 0.0476 and 0.0379). The optimized batch F10 showed a particle size of 167.1 nm, -19.5 mV zeta potential, and an entrapment efficiency of 87.32%. The optimized batch F10 was lyophilized and analyzed by Scanning electron microscopy (SEM), which showed a particle size of 130 nm. The solid powder was filled into the capsule for oral delivery.

Conclusion::

The marked improvement in solubility and bioavailability was achieved with F10- loaded Apixaban via Solid lipid nanoparticles. Moreover, the sustained released profile also minimizes the unseen complications that occur due to the clotting of blood.

01 Mar 2025·CURRENT PHARMACEUTICAL DESIGN

Establishment of an Integrated Population Pharmacokinetic/Pharmacodynamics Model of Apixaban in Chinese Healthy Population Adjusting for Key Genetic Variants

Article

Author: Zhao, Xia ; Bao, Jiachun ; Liao, Maoxing ; Cui, Yimin ; Xiang, Qian ; Wang, Zining ; Mu, Guangyan ; Zhou, Shuang ; Meng, Xianmin ; Hu, Kun ; Liu, Yaou ; Wang, Zhe ; Liu, Zhiyan ; Zhang, Hanxu ; Song, Jinfang ; Xie, Qiufen

Aims::

To improve the understanding of pharmacokinetic/pharmacodynamic (PK/PD) profiles of apixaban, supporting personalised drug prescriptions for future patients.

Background::

Genetic as well as nongenetic factors can affect the predictable PK and PD characteristics of apixaban.

Objective::

Establish a integrated popPK/PD model that adjusts for critical genetic variant.

Methods::

The integrated PK/PD models was characterized on the basis of PK (apixaban blood concentration) and PD (prothrombin time (PT), activated partial thromboplastin time (APTT), and anti-FXa activity) data from 181 healthy Chinese volunteers. Other investigated covariate variables included: Meaningful intrinsic and extraneous determinants, correlated genetic factors (ABCG2, F13A1, C3, etc.). A total of 2877 PK concentration observations were included in the modeling dataset.

Results::

The PK model of apixaban is adopted by single compartment model with first-order oral absorption. The estimated values of total clearance rate (CL/F), apparent distribution volume (V/F), and absorption rate constant (KA) in the final model are 3.37 L/h, 28.2 L, and 0.781 1/h, respectively. The PK model includes significance covariates such as FOOD, RBC, WT, and gene (ABCG2). The PD model of apixaban is adopted by a linear direct effect model with additive error, which was used to describe the relationship between markers such as APTT, PT, anti-FXa, versus plasma concentration. PK simulation within the modelled dose range is similar to clinical real date, while PD simulation results also show that the simulated exposure parameters is within the range of the literature.

Conclusion::

We established a comprehensive PK/PD model and used it to simulate markers level such as APTT, PT, and anti-FXa of apixaban. Individual predictive values with a dose of 2.5 mg are basically within the expected recommended range.

01 Feb 2025·Vascular and Endovascular Surgery

Axillary to Lateral Above Knee Popliteal Artery Bypass: An Alternative Approach to Lower Extremity Revascularization

Article

Author: Tenewitz, Paul ; Shames, Murry ; Parikh, Rajavi ; Nguyen, Trung

Objective:

Management of limb ischemia in the setting of malignancy with history of resection and/or radiation presents a unique challenge. Radiation arteritis contributing to limb ischemia may not respond to endovascular intervention. Furthermore, significant tissue scarring from extensive resection and/or radiation can increase the risk of complications with open intervention and limit revascularization options. Utilization of an axillary to popliteal artery bypass using a lateral approach to the popliteal artery has been described as a reasonable alternative in these challenging cases.

Case Report:

The patient is a 68-year-old male with history of liposarcoma of the left groin, scrotum, and medial thigh for which he underwent multiple resections, flap reconstruction, and skin graft. He had a recurrence 2 years later and underwent repeat resection, placement of brachytherapy catheters, vertical rectus abdominal flap, and external beam radiation. He now presents with Rutherford 2B acute limb ischemia with associated left foot drop. Computed tomography angiography was performed and revealed an occluded left common femoral artery stent, proximal left superficial and deep femoral artery occlusion, and thrombosis of the left femoral vein. An attempt was made at endovascular recanalization without success. He subsequently underwent left axillary-to-lateral above knee popliteal artery bypass with a 6 mm ringed polytetrafluoroethylene graft, tibial thrombectomy, and 4 compartment fasciotomy.

Results:

Post-operatively, his pain resolved. He continued to have left foot drop but recovered his ability to ambulate with a walker. He was ultimately discharged on post-operative day 11 to an inpatient rehabilitation facility on aspirin and apixaban.

Conclusion:

Hostile groin secondary to infection, malignancy requiring resection/radiation presents a unique challenge for revascularization. When endovascular revascularization or obturator bypass are not feasible options, axillary-to-lateral above knee popliteal artery bypass is a described, feasible alternative approach to restore blood flow in this challenging patient population.

189

News (Medical) associated with Apixaban

19 Nov 2024

·endpts.com

Ahead of adcomm, FDA raises safety questions for AstraZeneca’s reversal agent for life-threatening bleeds

The FDA on Thursday will convene an advisory committee to discuss the safety and efficacy of AstraZeneca’s Andexxa, which won accelerated approval in 2018 to reverse the anticoagulation effects of blood thinners that can cause life-threatening bleeding. The Cellular, Tissue, and Gene Therapies Advisory Committee will discuss the results of the confirmatory trial for the treatment. Also known as andexanet, it improved upon the standard of care but also revealed some safety issues and other concerns, FDA said in briefing documents released on Tuesday. The committee isn’t scheduled to vote on a recommendation. “Although andexanet showed superiority of the primary efficacy endpoint over UC [usual care] within the PEP [primary efficacy population], the superior efficacy at 12 hours did not predict longer-term benefit,” FDA said in its document. The FDA wants to hear more from the committee about increased rates of dangerous clotting and clotting-related deaths seen in a trial of Andexxa, compared with a standard of care reversal agent. And it’s looking for more discussion of the clinical meaningfulness of the benefit of Andexxa, and whether the benefit shown in the trial “outweighs the serious risks.” The treatment, a recombinant modified human factor Xa protein, is for patients treated with rivaroxaban or apixaban when rapid reversal of anticoagulation is needed because of life-threatening or uncontrolled bleeding. That could include, for example, when a patient needed urgent surgery because of a medical emergency or accident. Last year, AstraZeneca began plans to shift Andexxa to a full approval from its accelerated approval after halting its confirmatory trial early due to these efficacy findings. But FDA explained how the confirmatory trial, known as ANNEXA-I, revealed “major safety findings” including a “doubling of the rate of thromboses and thrombosis related deaths at Day 30 in the andexanet arm compared with” a standard of care clotting agent known as a prothrombin complex concentrate. Of the 239 patients treated with andexanet, FDA said, 14.6% of patients suffered thrombotic events versus 6.9% in the standard of care arm. While Andexxa demonstrated a statistically significant improvement in hemostasis, or the process to stop bleeding, compared with standard care, the agency also said that the “observed treatment difference between arms appears to be primarily driven by hematoma volume, with more patients in the andexanet arm compared to UC arm experiencing a ≤35% increase from baseline in hematoma volume at 12 hours (74% versus 60%).”

Drug ApprovalClinical ResultAccelerated Approval

19 Nov 2024

·www.prnewswire.com

TAHO Pharmaceuticals Initiates U.S. Phase III Clinical Trial of TAH3311 Antithrombotic Oral Dissolving Film, Dosing First Subjects

TAIPEI, Nov. 19, 2024 /PRNewswire/ -- TAHO Pharmaceuticals Ltd. announced the dosing of the first subjects in its U.S. Phase III clinical trial for its lead product, TAH3311, an innovative antithrombotic oral dissolving film (ODF). In July 2023, the U.S. Food & Drug Administration (FDA) accepted TAHO's proposal for a 505(b)(2) NDA submission, based on a single pivotal bioequivalence study comparing the plasma concentration of TAH3311 to the approved tablet formulation. This pivotal, open-label, randomized, crossover trial will enroll 60 subjects. TAH3311 introduces a groundbreaking ODF formulation of apixaban, a widely recognized first-line treatment and gold standard for stroke prevention and thrombosis management. Dr. Howard Lee, Chairman and CEO of TAHO Pharmaceuticals, stated: "Our team at TAHO Pharmaceuticals is dedicated to developing 505(b)(2) new drug formulations to address the clinical disadvantages of existing medications. Apixaban, available exclusively in tablet form, often presents challenges for elderly patients, children, and stroke survivors who have difficulty swallowing. These patients frequently need to crush tablets, mix them with water, and administer them twice daily—a time-consuming and imprecise process that risks dosage loss. TAH3311 overcomes these barriers with a quick-dissolving oral film that melts on the tongue, requires no water, reduces the risk of choking, enhances patient adherence, and alleviates caregiver burden." By addressing the clinical limitations of the tablet form and leveraging the significant market potential of apixaban, TAHO Pharmaceuticals is advancing TAH3311 as a meaningful innovation in anticoagulant therapy. About Apixaban Apixaban (co-developed by BMS and Pfizer under the brand name Eliquis®) is a direct factor Xa inhibitor and has been approved for clinical use in several thromboembolic disorders, including reduction of stroke risk in non-valvular atrial fibrillation, thromboprophylaxis following hip or knee replacement surgery, the treatment of deep vein thrombosis or pulmonary embolism, and prevention of recurrent deep vein thrombosis and pulmonary embolism. With notable safety advantages, it is the leading novel oral anticoagulant (NOAC). According to various industry reports, apixaban was the second-highest-selling drug globally in 2023. About TAHO Pharmaceuticals Ltd. Founded in 2010, TAHO Pharmaceuticals Ltd. leverages its proprietary Transepithelial Delivery System (TDS) to overcome the limitations of existing drugs and develop innovative dosage forms for niche markets. The TDS platform combines advanced transdermal and transmucosal delivery technologies, enabling the development of unique dosage forms such as transdermal patches, ODF, and buccal films. TAHO's diverse product portfolio spans a variety of therapeutic areas, including antithrombotic agents, opioid overdose antidotes, addiction treatments, pediatric ADHD, and chemotherapy-induced antiemetics. Among its notable achievements, TAH4411, an ODF for chemotherapy-induced nausea and vomiting, became the first product of its kind to receive regulatory approval and be commercialized in Japan. Media Contact: TAHO Pharmaceuticals +886-2-2659-8515 [email protected] SOURCE Taho Pharmaceuticals WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Phase 3NDADrug Approval

18 Nov 2024

·www.drugs.com

Certain Painkillers Can Raise Bleeding Risks for People on Blood Thinners

MONDAY, Nov. 18, 2024 -- People on blood thinners have a doubled risk of dangerous internal bleeding if they also take a non-steroidal anti-inflammatory drug (NSAID) like ibuprofen or naproxen, a new study warns. People typically are prescribed blood thinners to treat or prevent strokes , heart attacks, or blood clots in the legs or lungs, researchers said. NSAIDs also are known to thin the blood, and the new study shows that they can increase risk of uncontrolled bleeding in the gut, brain, lungs and bladder if taken alongside a blood thinner. “We found that for patients taking blood thinners for blood clots in the legs or lungs, using NSAIDs doubled the risk of bleeding compared with not using NSAIDs,” said researcher Soren Riis Peterson , a medical student with Aarhus University Hospital in Denmark. “The increased bleeding risk associated with NSAID use was not limited to the digestive tract but also seemed to affect other organ systems.” For the study, researchers analyzed data on nearly 52,000 Danish patients prescribed a blood thinner to treat a blood clot between 2012 and 2022. In Denmark, the NSAIDs diclofenac and naproxen can only be obtained through a prescription. This allowed researchers to track the health of patients who had been prescribed both a blood thinner and an NSAID. Overall, the risk of a bleed was two times higher when people took a blood thinner and an NSAID, compared to just taking a blood thinner, researchers found. The specific risk was four times higher for naproxen, three times higher for diclofenac and nearly twice as high for ibuprofen. Specific bleed risks included: Using NSAIDs with a blood thinner also tripled a person’s risk of anemia, researchers found. The pattern of risk remained similar across a wide variety of blood thinners, including rivaroxaban , apixaban , dabigatran , edoxaban and warfarin , results show. The new study was published Nov. 17 in the European Heart Journal . “For people taking blood thinners for blood clots in their legs or lungs, our research highlights the importance of being cautious when considering NSAIDs for pain or inflammation,” Petersen concluded in a journal news release. “We recommend that patients consult their doctor before taking NSAIDs along with a blood thinner.” In an accompanying editorial, Dr. Robert Storey , a professor of clinical cardiology with the University of Sheffield in the U.K., noted that NSAIDs are widely used, making up about 8% of prescriptions worldwide and often available over-the-counter. “It seems clear that avoiding NSAIDs in combination with [blood thinners] is the safest strategy to avoid excess bleeding risk,” Storey wrote. “However, if this is not possible, what mitigation can be put in place? NSAID prescription should obviously be at the lowest dose and for the shortest time possible, but choice of agent and route may also be important.” Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

AHA

100 Deals associated with Apixaban

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KEGG	Wiki	ATC	Drug Bank
D03213	Apixaban	B01AF02	DB06605

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Recurrent deep vein thrombosis	EU	Accord Healthcare SLU	23 Jul 2020
Recurrent deep vein thrombosis	IS	Accord Healthcare SLU	23 Jul 2020
Recurrent deep vein thrombosis	LI	Accord Healthcare SLU	23 Jul 2020
Recurrent deep vein thrombosis	NO	Accord Healthcare SLU	23 Jul 2020
Thrombosis	CN	Bristol-Myers Squibb/Pfizer EEIG	22 Jan 2013
Ischemic stroke	JP	Bristol-Myers Squibb KK	25 Dec 2012
Systemic embolism	AU	Bristol Myers Squibb Co.	21 Jul 2011
Atrial Fibrillation	EU	Bristol-Myers Squibb/Pfizer EEIG	18 May 2011
Atrial Fibrillation	IS	Bristol-Myers Squibb/Pfizer EEIG	18 May 2011
Atrial Fibrillation	LI	Bristol-Myers Squibb/Pfizer EEIG	18 May 2011
Atrial Fibrillation	NO	Bristol-Myers Squibb/Pfizer EEIG	18 May 2011
Embolism	EU	Bristol-Myers Squibb/Pfizer EEIG	18 May 2011
Embolism	IS	Bristol-Myers Squibb/Pfizer EEIG	18 May 2011
Embolism	LI	Bristol-Myers Squibb/Pfizer EEIG	18 May 2011
Embolism	NO	Bristol-Myers Squibb/Pfizer EEIG	18 May 2011
Pulmonary Embolism	EU	Bristol-Myers Squibb/Pfizer EEIG	18 May 2011
Pulmonary Embolism	IS	Bristol-Myers Squibb/Pfizer EEIG	18 May 2011
Pulmonary Embolism	LI	Bristol-Myers Squibb/Pfizer EEIG	18 May 2011
Pulmonary Embolism	NO	Bristol-Myers Squibb/Pfizer EEIG	18 May 2011
Stroke	EU	Bristol-Myers Squibb/Pfizer EEIG	18 May 2011

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Chronic Limb-Threatening Ischemia	Phase 3	BR	Wyeth AB	09 Jan 2020
Brain Infarction	Phase 3	US	Pfizer Inc.	19 Dec 2018
Brain Infarction	Phase 3	US	Bristol Myers Squibb Co.	19 Dec 2018
Cognitive Dysfunction	Phase 3	US	Bristol Myers Squibb Co.	19 Dec 2018
Cognitive Dysfunction	Phase 3	US	Pfizer Inc.	19 Dec 2018
Neoplasms	Phase 3	AT	Bristol Myers Squibb Co.	11 Oct 2018
Neoplasms	Phase 3	BE	Bristol Myers Squibb Co.	11 Oct 2018
Neoplasms	Phase 3	CA	Bristol Myers Squibb Co.	11 Oct 2018
Neoplasms	Phase 3	FR	Bristol Myers Squibb Co.	11 Oct 2018
Neoplasms	Phase 3	GR	Bristol Myers Squibb Co.	11 Oct 2018

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASH2024	Not Applicable	Thromboembolism	-	Prophylactic dose apixaban (2.5 mg twice daily)	dlrgfbpdyr(lpnkpzuuic) = ecqyxkvxud scnqevwgpt (salxfidtdv, 6.4 - 12.6) View more	-	08 Dec 2024
				Therapeutic dose apixaban (5 mg twice daily)	dlrgfbpdyr(lpnkpzuuic) = tebqxlkcqi scnqevwgpt (salxfidtdv, 14.8 - 19.8) View more
ASH2024	Not Applicable	Obesity, Morbid	-	Apixaban 2.5mg bid	supsfgexvm(qlmuexcktr) = iodokzazdh gcpvkrarsh (doppfvtmpv, ±5.4) View more	-	08 Dec 2024
NCT02464969 (B0661037, ASH2024)	Phase 4	Venous Thromboembolism	229	Apixaban	yvjgfnzkvp(ankabmqdrn) = pjtgizaxap urbtiiadeh (qtftlaayge, 0.8 - 6.7) View more	Positive	07 Dec 2024
				Standard of Care (VKA, LMWH, UFH)	yvjgfnzkvp(ankabmqdrn) = bmnigvtrid urbtiiadeh (qtftlaayge, 0.2 - 9.9) View more
NCT04865978 (DOAC LVAD, CTgov)	Phase 2	Heart Failure	30	LVAD implant+Apixaban (Apixaban)	cmqzsgxrqm(egcykszstp) = exargzthpu cceqowidqe (mxeleuzalz, qjnobwhtib - aoyssjopgd) View more	-	14 Nov 2024
				LVAD implant+Warfarin (Warfarin)	cmqzsgxrqm(egcykszstp) = kmxdwdwlaz cceqowidqe (mxeleuzalz, zrolcaxpve - hsvmrjbmar) View more
ESC2024	Not Applicable	Atrial Fibrillation	-	On-label standard dose (5mg twice daily)	zymaarrwmr(kwqfzyjphs) = kxazeldjrs gtyrczrain (dpcxnnoyci )	-	02 Sep 2024
				Off-label reduced-dose (2.5mg twice daily)	zymaarrwmr(kwqfzyjphs) = tlobjynrds gtyrczrain (dpcxnnoyci )
ESC2024	Not Applicable	Venous Thromboembolism	-	High dose Apixaban or Rivaroxaban	endjgpsuyd(xjjkdoajtr) = sncvdcaqjx dridjdwsck (kftyzdtkdz ) View more	-	30 Aug 2024
				Standard dose Apixaban or Rivaroxaban	endjgpsuyd(xjjkdoajtr) = xejzjkchlz dridjdwsck (kftyzdtkdz ) View more
NCT04974684 (CTgov)	Not Applicable	-	45	Apixaban (Apixaban Alone Group)	lpuuaojhay(edatnjhyxl) = ebwnhptdsn emoityjlum (fsqxejdnyj, klkrbsmymw - yjnwvgionk) View more	-	20 Aug 2024
				Apixaban+Aspirin (Apixaban + Aspirin Group)	lpuuaojhay(edatnjhyxl) = osnejdijjj emoityjlum (fsqxejdnyj, abexstrkqp - vkyahwdlxf) View more
NCT01938248 (ARTESiA, Pubmed \| J Am Coll Cardiol)	Phase 4	Stroke \| Embolism and Thrombosis \| Atrial Fibrillation	-	Apixaban	ddpqidutyw(rfmbxghzwr) = lktnnkqkxr zqpncriymw (zaaicqiuvv )	Positive	23 Jul 2024
				Aspirin	ddpqidutyw(rfmbxghzwr) = idjlougmsk zqpncriymw (zaaicqiuvv )
ASCO2024	Not Applicable	Multiple Myeloma IMiD treatment	448	Apixaban	pnrzxaqyld(xdlnhcmogg): HR = 0.7 (95% CI, 0.56 - 0.88) View more	Positive	24 May 2024
				Warfarin
SAVED and IMPEDE VTE (ASCO2024)	Not Applicable	Multiple Myeloma SAVED score \| IMPEDE score	347	Aspirin	weuhvtjnnc(ulrfzxjbhn) = ecjxvetvvq dddhovpjbe (kdnplbspww )	Positive	24 May 2024
				Apixaban	weuhvtjnnc(ulrfzxjbhn) = ryxxbbsyxv dddhovpjbe (kdnplbspww )