In the current literature, infection with the hepatitis B virus (HBV) is described as one of the main risk factors for the development of hepatocellular carcinoma (HCC).
According to the current study situation, the Hepatitis B surface antigen (HBsAg) is considered as an important marker, since low levels and sero-clearance of HBsAg are both correlated with a lower risk of HCC development / recurrence.Currently there is no treatment option available that efficiently targets HBsAg. Besides neutralizing infectious HBV virions, Hepatitis B immunoglobulins (HBIG) can directly bind and neutralize extracellular HBsAg/SVPs, and even intracellular HBsAg targeting is reported. In addition, HBIGs can initiate effector-cell attack (via antibody-dependent cellular cytotoxicity, ADCC) towards infected hepatocytes.
The potential benefit of HBIGs in the HCC context is further underlined by recent evidence for the ability of HBIGs to reduce the viability, proliferation, and self-renewal of tumor-initiating cells (TICs) - isolated from HBV-HCC patients - accompanied by downregulation of stemness markers, e.g., OCT-4.According to the current study situation, the use of HBIGs significantly reduces the risk of HBV reinfection after transplantation and improves the results of liver transplantation in patients with chronic HBV infection. The potential benefit of treating HBV-HCC patients on the LTx (liver transplantation) waiting list with hepatitis B immunoglobulin is the possible stop or inhibition of tumor progression while waiting for an LTx. So far there is no clinical evidence of this.
Mechanistically, hepatitis B immunoglobulin could occur through neutralization of circulating HBsAg, which is an important driver of an immunosuppressive environment in HBV patients, and possibly through direct effects against HBV HCC tumor cells (through antibody-dependent cellular cytotoxicity, ADCC). Therefore, the idea behind preoperative HBIG administration before liver transplantation is to reduce the rate of patients in whom a transplantation would no longer have been possible due to tumor progression. Thus, due to tumor progression in HBV-positive HCC-patients there is a monthly drop-out from the waiting list of about 4%.
The basic idea behind the treatment of HBV-HCC patients before tumor resection with hepatitis B immunoglobulin is to potentially stop or positively influence tumor progression through the effects mentioned above, in the time between diagnosis and resection.
Zhou et al. (2015) have shown a connection between HBsAg levels and HCC relapses after resection, although the exact role of HBsAg is still unclear. In no case will the treatment postpone the time of tumor resection, as only patients are considered who, for clinical reasons, can expect a certain time until resection. The present proof of concept study aims to quantify HBsAg reduction due to preoperative administration of HBIGs in HBV-positive HCC-patients and serve as a template for future multicentre clinical trials.

Start Date01 Nov 2024

Sponsor / Collaborator

Medizinische Universität Graz

NCT04629651

/ WithdrawnPhase 1/2IIT

Phase I/II Prospective Trial Investigating the Safety and Efficacy of Captopril Use on the Degree of Marrow Fibrosis in Patients With Primary or Secondary Bone Marrow Fibrosis/Myeloproliferative Neoplasms

The purpose of this study is to evaluate the safety and tolerability of captopril and evaluate the effectiveness captopril as measured by changes in the grade of bone marrow scar tissue. The change in spleen size by ultrasound will also be measured.

Start Date01 Apr 2024

Sponsor / Collaborator

The Case Comprehensive Cancer Center

NCT06292091

/ CompletedPhase 1IIT

An Open-label, Fixed-sequence, 3-period Crossover Exploratory Study to Investigate the Effect of Urine Acid-base Disequilibrium on the Pharmacokinetics of Captopril in Healthy Male Volunteers

The aim of this study is to evaluate the effect of urine acid-base disequilibrium on the pharmacokinetics of captopril in healthy male volunteers.

Start Date28 Feb 2024

Sponsor / Collaborator

Seoul National University Hospital

100 Clinical Results associated with Captopril

100 Translational Medicine associated with Captopril

100 Patents (Medical) associated with Captopril

21,851

Literatures (Medical) associated with Captopril

01 May 2025·Journal of Photochemistry and Photobiology A: Chemistry

Assessing the stability and reactive oxygen species generation of thiolate-protected nanoclusters in physiological conditions

Author: Stamplecoskie, Kevin G. ; Aminfar, Parimah ; Harrington, Kristen

Gold and silver nanoclusters have emerged as next generation bioimaging and cancer therapy agents, based on the potent effects that nanoclusters have in cell and animal models.However, understanding how nanocluster structure and properties are affected by the chem. environment of the body and tumor-like conditions is far less explored.Here, the stability of six different clusters with varied metals (Au or Ag) and ligands were investigated to elucidate the impact that each has on cluster stability in physiol. conditions and in a solution that mimic cellular environment surrounding the tumor.Surprisingly, the most studied Au₂₅(SR)₁₈ superatom clusters were not stable in physiol. media, whereas a newly reported cluster, Au₂₂(lysine-cysteine-lysine)₁₆, showed 24-h stability in all conditions studied.The ability to generate reactive oxygen species under the same conditions was also assessed, identifying several clusters as good candidates for use in photodynamic therapy.

01 Mar 2025·Osteoporosis International

Osteoporotic fracture risks of thiazides and dihydropyridines in angiotensin modulator users

Article

Author: Lin, Yang-Chi ; Huang, Jing-Yang ; Chiang, Ping-Hao ; Wu, Wen-Shiann

This study examined the impact of thiazide and RAAS antihypertensive medications vs DHP-RAAS medications on fracture risk. The close alignment of such settings with clinical use, combined with the potential bone benefits of ACEis and ARBs, provides enhanced accuracy in bone health evidence.PURPOSETo determine whether thiazides, combined with either angiotensin-converting enzyme inhibitor (ACEi) or angiotensin II receptor blocker (ARB), offer bone-protective benefits compared with dihydropyridine (DHP) drugs combined with ACEi or ARB.METHODSThis retrospective cohort study was conducted on the US Collaborative Network from the TriNetX database on March 5th, 2024. It included hypertensive ACEi or ARB users under thiazide or DHP drug treatments spanning from January 1st, 2015, to December 31st, 2022, with exclusion criteria applied. The primary outcome is a composite typical osteoporotic fracture (TOPF). Kaplan Meier analyses were performed after 1:1 propensity-score matching (PSM) with a 5-year follow-up. Besides investigating fracture-related outcomes in thiazide-ACEi/ARB and DHP-ACEi/ARB users, this study explores whether the effects differ between ACEi and ARB users. Subgroup analyses were also performed, and the heterogeneity among the results was assessed using Cochran's Q-tests.RESULTSPost-PSM results yield 54,240 patients per cohort in the primary analysis, aging 61.5 ± 12.2 versus 61.4 ± 13.7 (thiazide-ACEi/ARB versus DHP-ACEi/ARB) with predominantly white ethnicity. Thiazide-ACEi/ARB users exhibit lower TOPF risk than DHP-ACEi/ARB users (hazard ratio (HR) = 0.65, 95% confidence interval (CI) 0.61-0.70), and such benefits from thiazides are similar between ACEi and ARB users (ACEi: HR = 0.69; ARB: HR = 0.67, Cochran's Q-test p-value = 0.78). Additionally, the effects of thiazides reveal significant heterogeneity between patients with and without inflammatory polyarthropathy (ICD-10, M05-M14) and benzodiazepine usage (Cochran's Q-test p-value = 0.01, 0.04).CONCLUSIONThiazides are associated with lower risks of typical osteoporotic fractures compared to DHP drugs in patients treated with ACEi or ARB, while such benefits may diminish in those with a diagnosis of inflammatory polyarthropathy and benzodiazepine usage.

01 Mar 2025·Psychopharmacology

Captopril attenuates oxidative stress and neuroinflammation implicated in cisplatin-induced cognitive deficits in rats

Article

Author: Mantawy, Eman M ; Said, Riham S ; El-Demerdash, Ebtehal ; Azab, Samar S ; Mostafa, Fatma

AbstractRationaleOne of the most debilitating drawbacks of cisplatin chemotherapy is neurotoxicity which elicits memory impairment and cognitive dysfunction (chemobrain). This is primarily triggered by oxidative stress and inflammation. Captopril, an angiotensin-converting enzyme inhibitor, has been reported as a neuroprotective agent owing to its antioxidant and anti-inflammatory effects.ObjectiveWe examined the possible neuroprotective effect of captopril against cisplatin-induced neurological and behavioral abnormalities in rats.MethodsChemobrain was induced in rats by cisplatin (5 mg/kg, i.p.) on the 7th and 14th days of the study while captopril was administered orally (25 mg/kg) daily for three weeks. The effects of captopril were assessed by performing behavioral tests, histological examination, and evaluation of oxidative stress and inflammatory markers.ResultsCisplatin caused learning/memory dysfunction assessed by passive avoidance and Y-maze tests, decline in locomotion, and rotarod motor balance loss which were further verified by neurodegeneration observed in histological examination. Also, cisplatin aggravated oxidative stress by elevating lipid peroxidation (MDA) levels and diminishing catalase activity. Moreover, cisplatin upregulated the neuroinflammatory markers (TNF, IL-6, GFAP, and NF-κB). Captopril successfully ameliorated cisplatin damage on the levels of neurobehavioral and histopathological changes. Mechanistically, captopril significantly diminished MDA production and preserved catalase antioxidant activity. Captopril also counteracted neuroinflammation through inhibiting NF-κB and its downstream proinflammatory cytokines besides repressing astrocyte activity by reducing GFAP expression.ConclusionOur findings revealed that captopril could abrogate cisplatin neurotoxicity via reducing oxidative stress and neuroinflammation thus enhancing cognitive and behavioral performance. This could suggest the repurposing of captopril as a neuroprotective agent, especially in hypertensive cancer patients receiving cisplatin.

News (Medical) associated with Captopril

21 Jun 2024

·www.drugs.com

Angiotensin Receptor Blocker Use Linked to Lower Incidence of Epilepsy

FRIDAY, June 21, 2024 -- For patients with hypertension, angiotensin receptor blockers (ARBs) are associated with a reduced incidence of epilepsy compared with other antihypertensive medications, according to a study published online June 17 in JAMA Neurology . Xuerong Wen, Ph.D., from the University of Rhode Island in Kingston, and colleagues conducted a retrospective cohort study to examine the association between ARB use and epilepsy incidence in subgroups of U.S. patients with hypertension. Patients who received ARBs were propensity score (PS)-matched to those who received angiotensin-converting enzyme inhibitors (ACEIs), β-blockers, calcium channel blockers (CCBs), or a combination of these medications. Of the participants, 309,978 received ARBs, 807,510 received ACEIs, 695,887 received β-blockers, and 448,589 received CCBs; the 1:1 PS-matched subgroups included 619,858 patients for ARB versus ACEI, 619,828 patients for ARB versus β-blocker, and 601,002 patients for ARB versus CCB. The researchers found that the incidence of epilepsy was reduced with use of ARBs versus ACEs, β-blockers, and a combination of other antihypertensive classes (adjusted hazard ratios, 0.75, 0.70, and 0.72, respectively). In subgroup analyses, the investigators observed a significant association between ARB use (mainly losartan) and epilepsy incidence in patients with no preexisting history of stroke or cardiovascular disease. "Further pharmacological studies, including randomized clinical trials, are needed to establish antiepileptogenic properties of antihypertensive medications," the authors write. Two authors disclosed ties to the pharmaceutical and medical device industries.

Clinical Result

14 May 2024

·www.prnewswire.com

CardioPharma Announces Issuance of Global Patent to Mitigate the World's Top Killer

WILMINGTON, N.C., May 14, 2024 /PRNewswire/ -- CardioPharma Inc. (the "Company"), a specialty pharmaceutical company focused on drug development for cardiovascular diseases, announced that on August 29, 2023, the United States Patent and Trademark Office ("USPTO") issued US Patent 11,737,988 B2 entitled "Anti-Hypertensive and Cholesterol-Lowering Fixed-Dose Combination and Method of Manufacture." Additional patents covering the subject matter of the '988 Patent have been granted in South Africa in 2022 and Australia, Armenia, Belarus, and the Russian Federation in 2024. Three further patents have been accepted in Canada, New Zealand, and Israel and will issue in the near future. In addition to the foregoing, CardioPharma is pursuing additional patents in major markets throughout the world, all of which together will bolster CardioPharma's global presence for the products covered by the patent grants. The 20-year term for all of the patents runs through April 17, 2039. CardioPharma Pipeline CardioPharma's pipeline products contain some of the world's most consumed, individually dispensed medications for the prevention and treatment of cardiovascular disease. The lead product, CardiaPill® is a unique formulation combining a cholesterol modifying agent ("statin"), an Angiotensin-converting-enzyme inhibitor (ACE Inhibitor) and anti-platelet agent. Statins moderate cholesterol levels and include products such as Lipitor®, Zocor®, Pravachol®; and Crestor®. ACE inhibitors reduce blood pressure and include products such as Altace®, Lotensin®, Capoten® and Accupril®. Pipeline products also include combinations using Angiotensin II Receptor Blockers (ARBs) as well as different statins and other anti-platelet agents. Simplicity of dosing, improved adherence and significant cost benefits for patients, providers and payors around the world are among the many compelling and well-documented benefits that make these inexpensive products so anticipated. About CardioPharma CardioPharma (), Inc. is a specialty pharmaceutical company focused on patent-protected combinatorial cardiovascular medications. CardioPharma's goal is to create drugs that make it easier and more cost-effective for doctors and their patients to reduce the morbidity and mortality of the world's number one killer – cardiovascular disease. The products are unique to the global pharmaceutical industry – highly cost-effective with proven efficacy; providing both patient and provider convenience; promoting adherence, while delivering superior clinical outcomes and economic benefits to all stakeholders. For more information, visit . Forward looking statements The information in this press release contains forward-looking statements including the prospective development, commercialization and regulatory approval in the U.S. and international markets. Words such as "expects," "plans," "believe," "may," "will," "anticipated," "intended" and variations of these words or similar expressions are intended to identify forward-looking statements. In addition, any statements that refer to expectations, projections or other characterizations of future events or circumstances, including any underlying assumptions, are forward-looking statements. These statements are not guarantees of future performance and are subject to risks, uncertainties and assumptions that are difficult to predict. Therefore, our actual results could differ materially and adversely from those expressed in any forward-looking statements as a result of various factors including the Company's ability to raise sufficient funds to bring new products to the global market. Contact: [email protected] SOURCE CardioPharma, Inc.

Patent Expiration

04 Sep 2023

·synapse.patsnap.com

ACE inhibitor -Overview of its R&D Progress | Competitive Landscape | Key Drug

ACE, or angiotensin-converting enzyme, plays a crucial role in the human body by regulating blood pressure and fluid balance. It converts angiotensin I, a hormone produced by the liver, into angiotensin II, a potent vasoconstrictor that narrows blood vessels. This process increases blood pressure and stimulates the release of aldosterone, a hormone that promotes sodium and water retention. ACE also breaks down bradykinin, a peptide that causes blood vessels to dilate and lowers blood pressure. Due to its involvement in these important physiological processes, ACE inhibitors are commonly used in the treatment of hypertension, heart failure, and other cardiovascular conditions. ACE Competitive LandscapeAccording to the data provided by Patsnap Synapse-Global Drug Intelligence Database: the following figure shows that as of 2 Sep 2023, there are a total of 163 ACE drugs worldwide, from 159 organizations, covering 68 indications, and conducting 810 clinical trials. 👇Please click on the picture link below for free registration or login directly if you have freemium accounts, you can browse the latest research progress on drugs , indications, organizations, clinical trials, clinical results, and drug patents related to this target. The analysis of the target ACE reveals a competitive landscape with companies like Les Laboratoires Servier SAS, CHIESI Farmaceutici SpA, and Viatris Inc. leading in R&D efforts. The focus of research is primarily on indications like hypertension, heart failure, and cardiovascular diseases. Small molecule drugs dominate the market, but there is also potential in other drug types like peptide drug conjugates and monoclonal antibodies. The European Union, China, the United States, and Japan are the key regions driving the development of ACE-related drugs. China, in particular, has shown significant progress. Overall, the target ACE presents opportunities for further research and development, with potential for innovative drugs and intense competition in the market. Key Drug: CaptoprilCaptopril is a small molecule drug that targets ACE and is used in the treatment of various cardiovascular, endocrinology, and urogenital diseases. It has been approved for multiple indications, including essential hypertension, hypertensive nephropathy, heart failure, and myocardial infarction. This wide range of indications highlights the versatility and effectiveness of Captopril in managing different conditions related to the cardiovascular system and metabolic disorders. 👇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. Captopril was first approved in Japan in January 1980, making it a well-established drug with a long history of use. The drug has achieved the highest phase of approval both globally and in China, indicating its widespread acceptance and recognition by regulatory authorities. This suggests that Captopril has undergone rigorous testing and evaluation to ensure its safety and efficacy Enalapril MaleateEnalapril Maleate is a small molecule drug that primarily targets ACE. It is used in the treatment of various therapeutic areas including immune system diseases, infectious diseases, nervous system diseases, cardiovascular diseases, and urogenital diseases. The drug has been approved for the treatment of ventricular dysfunction, left, angina pectoris, myocardial infarction, encephalomyelitis, eastern equine, immune system diseases, heart failure, essential hypertension, hypertension, renal, hypertension, renovascular, and hypertension. 👇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. Enalapril Maleate has a long history of use since its first approval in 1985. Its broad therapeutic areas and indications make it a versatile drug in the field of biomedicine. The drug's approval in both the global and Chinese markets further solidifies its position as a widely recognized and accepted treatment option. As a small molecule drug targeting ACE, Enalapril Maleate plays a crucial role in managing various diseases and conditions, particularly those related to the immune system, cardiovascular system, and nervous system. LisinoprilLisinopril is a small molecule drug that falls under the therapeutic area of cardiovascular diseases. It primarily targets ACE and is used to treat various conditions related to the heart and blood vessels. The drug has been approved for use in multiple indications, including acute myocardial infarction, kidney diseases, chronic heart failure, hypertension, and heart failure. 👇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. Lisinopril was first approved in the United States in December 1987 and has been developed by Merck Sharp & Dohme Corp. and AstraZeneca PLC. Lisinopril has reached the highest phase of development, indicating its safety and efficacy, and has received regulatory approval both globally and in China.

100 Deals associated with Captopril

External Link

KEGG	Wiki	ATC	Drug Bank
D00251	Captopril	C09AA01	DB01197

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Essential Hypertension	Japan	Alfresa Pharma Corp.	07 Oct 1982
Hypertension, Malignant	Japan	Alfresa Pharma Corp.	07 Oct 1982
Hypertension, Renovascular	Japan	Alfresa Pharma Corp.	07 Oct 1982
Hypertensive Nephropathy	Japan	Alfresa Pharma Corp.	07 Oct 1982
Diabetic Nephropathies	Japan	Daiichi Sankyo Co., Ltd.	01 Jan 1980
Heart Failure	Japan	Daiichi Sankyo Co., Ltd.	01 Jan 1980
Hypertension	Japan	Daiichi Sankyo Co., Ltd.	01 Jan 1980
Myocardial Infarction	Japan	Daiichi Sankyo Co., Ltd.	01 Jan 1980

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03179163 (H2SPharm, CTgov)	Phase 1/2	Essential Hypertension	10	Captopril	xjsplmpbpz(dibkwwhjon) = yrkxiqknmo uyqmeslizq (ghvzqavvwv, qeuadrfqxu - isstdutlqw) View more	-	28 Feb 2024
ISN WCN2022	Not Applicable	Acute Tubulointerstitial Nephritis	1	Captopril	kkycxanbfa(nuiuqphwrp) = kamrnyuxcg aqpepurbmi (lnqmwzgewl ) View more	Positive	01 Feb 2022
NCT01669434 (CTgov)	Phase 4	Hypotension	291	LISINOPRIL+Captopril+ENALAPRILAT+BENAZEPRIL HYDROCHLORIDE+PERINDOPRIL ERBUMINE+RAMIPRIL+QUINAPRIL HYDROCHLORIDE+Enalapril Maleate+Perindopril Arginine+FOSINOPRIL SODIUM+TRANDOLAPRIL+MOEXIPRIL HYDROCHLORIDE (ACEI Omission)	jcihhttyrr(buoxbexkmp) = rbjoltuoob bfypkizvrn (bqlhxzvjdr, rbwocxpxba - ivhxrlqpff) View more	-	11 Dec 2017
				ACEI continuation (ACEI Continuation)	jcihhttyrr(buoxbexkmp) = perlqwtyrv bfypkizvrn (bqlhxzvjdr, iriglyroxa - rqypudjejg) View more
ASN2014	Not Applicable	Hypertension	-	Captopril	cxmzymmgey(yimesegxoa) = burgwravva yyvbokwqba (epscahfiul ) View more	-	11 Nov 2014
				Vehicle	cxmzymmgey(yimesegxoa) = yqlrbtaswv yyvbokwqba (epscahfiul ) View more
NCT00660309 (CTgov)	Phase 4	Diabetes Mellitus, Type 2	45	Captopril+Aliskiren (Aliskiren)	vxgqfgwijr(hivdkujmfq) = crbrlpeejx govmszzmvx (jzozuongvi, zvvizbdoil - svpjfcrpms) View more	-	29 Aug 2012
				Captopril+Irbesartan (Irbesartan)	vxgqfgwijr(hivdkujmfq) = fvdfjktvdg govmszzmvx (jzozuongvi, jgmqdabihx - rvgyhsssbl) View more
ARVO2012	Not Applicable	Diabetic Retinopathy	317	Captopril	cbldycbvca(bhlobuymcw) = zjpftnzqop gbymcanwft (npqxyhntgv ) View more	-	01 Mar 2012
				Vitamin C	cbldycbvca(bhlobuymcw) = hnvmdbdocb gbymcanwft (npqxyhntgv ) View more
ORAL SOLO (A3921045) (EULAR2011)	Phase 3	Rheumatoid Arthritis	610	CP 5 mg BID	(qpbevjfjoz) = vdqahhnsym fkntcuzbmv (curnrcmlvg )	Positive	25 May 2011
				CP 10 mg BID	(qpbevjfjoz) = lkjnpqgxsc fkntcuzbmv (curnrcmlvg )
ASN2010	Not Applicable	Bone marrow transplant rejection	-	Captopril	(lobyukoglm) = zwsdakxars vxrhhbyzwn (wmuqwncpha )	Positive	16 Nov 2010
				Captopril (No-drug group)	(lobyukoglm) = stktzmpmlg vxrhhbyzwn (wmuqwncpha )
ASN2010	Not Applicable	-	-	ACEIs	hjpfqrhzlc(zszyelcgop) = wunumxcont ftvwyoopqq (jlcoalyxid )	-	16 Nov 2010
				ARBs	jnljdustog(ukayytomrc) = sjjzpfooqb dpyvzlgzya (fehvyosyvv ) View more
EULAR2009	Not Applicable	Rheumatoid Arthritis	655	CP 5 mg BID	(zfesvkxmnl) = jmwyupjmuh jdqiysltmz (yajyyumfgj ) View more	-	10 Jun 2009

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