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Last update 15 Feb 2025

Simvastatin

Last update 15 Feb 2025

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

SummarySimvastatin, a diminutive molecular entity, functions as an HMG-CoA reductase enzyme inhibitor, which is accountable for the synthesis of cholesterol in the hepatic tissue. Classified as HMG-CoA reductase inhibitors or statins, it treats sundry ailments that result from elevated cholesterol levels. Simvastatin's active indications encompass heterozygous familial hypercholesterolemia, hyperlipoproteinemia Type V, stroke, hyperlipidemias, and hyperlipoproteinemia Type II. Merck Sharp & Dohme Corp. initially synthesized simvastatin, and it received the first nod for clinical use in 1988. In spite of its prevalent administration, simvastatin may elicit an array of side effects, for example, myalgia and hepatotoxicity, and patients should seek counsel from their medical practitioners before initiating its intake.

Drug Type

Small molecule drug

Synonyms

Simvastatin (JP17/USP/INN), Simvastatin for Suspension, Simvastatin Unlubricated Granulation

+ [44]

Target

HMGCR

Mechanism

HMG-CoA reductase inhibitors(HMG-CoA reductase inhibitors)

Therapeutic Areas

Nervous System DiseasesCardiovascular DiseasesCongenital Disorders+ [1]

Active Indication

Hyperlipoproteinemia Type VCoronary DiseaseHyperlipidemias+ [5]

Inactive Indication

Acute Coronary SyndromeAlzheimer DiseaseAtrial Fibrillation+ [9]

Originator Organization

Merck Sharp & Dohme Corp.

Active Organization

Organon & Co.

Salerno PharmaStartup

Hangzhou MSD Pharmaceutical Co. Ltd.

+ [1]

Inactive Organization

Merck Sharp & Dohme Corp.Synthon Pharmaceuticals, Inc.Merck Sharp & Dohme LLC

Drug Highest PhaseApproved

First Approval Date

AU (12 Sep 1991),

Coronary Artery DiseaseHeterozygous familial hypercholesterolemiaHypercholesterolemia+ [1]

Regulation-

Structure/Sequence

Molecular FormulaC25H38O5

InChIKeyRYMZZMVNJRMUDD-HGQWONQESA-N

CAS Registry79902-63-9

640

Clinical Trials associated with Simvastatin

NCT06785727

/ Not yet recruitingPhase 4IIT

StAtins in Frail OldEr Patients with Ischemic Stroke or Transient Ischemic Attack - the Randomized Controlled Trial

Two Dutch guidelines (Stroke and Cardiovascular Risk Management) provide conflicting advice on optimal statin treatment in older patients. In the SAFEST - RCT, the investigators will assess the impact of starting versus not starting a statin in frail individuals aged 70 and above with a recent ischemic stroke or transient ischemic attack (TIA) on their health-related quality of life and Major Adverse Cardiovascular Events (MACE) free survival during a two-year follow-up period.

Start Date01 Feb 2025

Sponsor / Collaborator

Academic Medical Center University of Amsterdam

[+1]

CTRI/2024/10/074804

/ Not yet recruitingPhase 3IIT

Comparison of the effect of Simvastatin impregnated gel foam and Platelet rich Fibrin on post-operative outcomes in patients undergoing extraction of mandibular molars - nil

Start Date15 Oct 2024

Sponsor / Collaborator-

IRCT20171015036782N10

/ RecruitingPhase 3IIT

Comparison of the quality of formed bone and pain after use of platelet rich fibrin (PRF) and Simvastatin in the extracted tooth socket

Start Date06 Oct 2024

Sponsor / Collaborator-

100 Clinical Results associated with Simvastatin

100 Translational Medicine associated with Simvastatin

100 Patents (Medical) associated with Simvastatin

18,843

Literatures (Medical) associated with Simvastatin

01 Apr 2025·SEPARATION AND PURIFICATION TECHNOLOGY

Using artificial neural networks to elucidate retention interactions on stationary phases with amine moieties dedicated to supercritical fluid chromatography

Author: Plachka, Katerina ; Plachká, Kateřina ; Gazarkova, Tatana ; Pilarova, Veronika ; Nováková, Lucie ; Pilařová, Veronika ; Svec, Frantisek ; Švec, František ; Garrigues, Jean-Christophe ; Novakova, Lucie ; Gazárková, Taťána

The retention mechanisms of small mols. on a wide range of stationary phases using different mobile phase compositions are one of the most discussed topics in current state-of-the-art supercritical fluid chromatog. (SFC).Although various theories have been published on retention behavior, prediction, and stability over time, an in-depth insight into the mechanisms is still lacking.Our study focused on the description of the retention mechanisms on columns with amine moieties, i.e., 2-ethylpyridine, 2-picolylamine, 1-aminoanthracene, and diethylamine, dedicated to SFC, using three different compositions of organic modifier, i.e., methanol, methanol + 10 mmol/L NH₃, and methanol + 2% H₂O, in CO₂.An extensive set of analytes characterized by more than 200 mol. descriptors was used.The importance of the effect of each mol. descriptor on the retention behavior was determined by artificial neural networks.Thus, the descriptors increasing and/or decreasing retention on individual columns using different mobile phase compositions were defined.The data collected over one year of column use were statistically evaluated to describe the retention behavior of small mols. on the tested stationary phases using three organic modifiers and to describe the changes in retention behavior over time.As the development of the SFC method can be laborious and time-consuming, this publication offers a detailed description of the interactions taking place between the analyte and the SFC stationary phase.Understanding these fundamental processes will enable faster development of SFC methods using quality-by-design principles.

01 Mar 2025·BIOCHEMICAL PHARMACOLOGY

Simvastatin and rosuvastatin attenuate necroptosis in rat failing hearts following myocardial infarction; the contribution of Hsp90 inhibition in cardiomyocytes to prevent necroptosis

Article

Author: Marunouchi, Tetsuro ; Sato, Kaho ; Murakami, Takuma ; Matsumura, Kasumi ; Tanonaka, Kouichi ; Takeuchi, Shiori

Statins, a class of dyslipidemic drugs known as HMG-CoA reductase inhibitors, have emerged as promising compounds for the treatment of chronic heart failure. Nevertheless, the precise mechanism remains to be fully elucidated. Necroptosis is a programmed necrosis-like cell death and has been involved in the development of chronic heart failure. However, it is unclear whether statins exert beneficial effects on therapy for heart failure by inhibiting cardiomyocyte necroptosis. In this study, we administered statins to rats after myocardial infarction and evaluated their effects on the necroptosis pathway in the failing heart following myocardial infarction. Administration of simvastatin or rosuvastatin reduced cardiac dysfunction after myocardial infarction. Concomitantly, the statins prevented the activation of the necroptotic intracellular signaling pathway in myocardial tissue. Simvastatin, but not rosuvastatin treatment attenuated the interaction between Hsp90 and necroptosis-related proteins in myocardial tissue, suggesting that simvastatin prevents necroptosis via Hsp90 inhibition. Necroptosis induced in primary cultured cardiomyocytes isolated from neonatal rats was inhibited by pretreatment with simvastatin. Administration of simvastatin and rosuvastatin inhibited the infiltration of M1 macrophages into myocardial tissue and reduced the myocardial tissue content of tumor necrosis factor-α, an inflammatory cytokine that induces necroptosis, respectively. The findings in the study indicate that statins may prevent necroptosis of cardiomyocytes, attenuating the development of heart failure. However, the present study suggests that the cardioprotective mechanism of simvastatin is not same as that of rosuvastatin.

01 Mar 2025·JOURNAL OF MOLECULAR STRUCTURE

Construction of a wavelength tunable supramolecular fluorescent probe for serum albumin-mediated live cell imaging

Author: Chang, Kai-Li ; Xu, Shao-Hu ; Qin, Wen-Xuan ; Wang, Qing ; Zhang, Jing

A wavelength-tunable supramol. fluorescent probe for live cell imaging mediated by serum albumin was successfully crafted, leveraging the assembly of host-guest complexes formed between water-soluble pillar[5]arene (WP5) and the N-heteroaromatic fluorescent probes DMM and DDM, resp.Both the complexes demonstrated selective responsiveness towards bovine serum albumin (BSA), accompanied by favorable BSA binding abilities and remarkable anti-interference properties in their BSA responsiveness.Notably, the WP5⊃DMM and WP5⊃DDM complexes shared these exceptional attributes, which were inherent to DMM and DDM, resp.Importantly, the formation of complexes with WP5 did not adversely impact their responsiveness or binding abilities to BSA.In response to BSA, the WP5⊃DMM and WP5⊃DDM complexes exhibited relatively fixed but distinct excitation and emission bands.Apart from this characteristic, these complexes displayed no significant differences in other properties, even when self-assembled into spherical supramol. fluorescent probes in aqueous solutionThus, it became feasible to achieve multicolor imaging in live cells mediated by serum albumin by adjusting the ratio of WP5⊃DMM and WP5⊃DDM complexes within the supramol. fluorescent probes.

News (Medical) associated with Simvastatin

13 Jan 2025

·www.prnewswire.com

Akebia Therapeutics Announces Multiple Positive Business Updates

New Commercial Supply Contracts for Vafseo® (vadadustat) secured, bringing availability and dialysis organization coverage to nearly 100% of patients on dialysis in U.S. Vafseo tablets now shipping in the U.S. Plan to start Phase 3 trial in mid-2025 to potentially expand Vafseo label to include treatment of late-stage non-dialysis CKD patients Company to discuss business updates at 43rd Annual J.P. Morgan Healthcare Conference CAMBRIDGE, Mass., Jan. 13, 2025 /PRNewswire/ -- Akebia Therapeutics®, Inc. (Nasdaq: AKBA), a biopharmaceutical company with the purpose to better the lives of people impacted by kidney disease, today announced multiple positive business updates. As of January, Vafseo® (vadadustat) tablets are available in the U.S. for adult patients with anemia due to chronic kidney disease (CKD) on dialysis for at least three months, and shipment of product to dialysis centers has commenced. In addition, Akebia recently signed a Vafseo commercial supply agreement with a leading dialysis organization. Akebia now has contracts in place with dialysis organizations caring for nearly 100% of dialysis patients in the U.S. As previously announced, Vafseo qualifies for the Transitional Drug Add-On Payment Adjustment (TDAPA) reimbursement as directed by the Centers for Medicare & Medicaid Services (CMS), and CMS has published billing guidance and reimbursement rates. Akebia also announced its plans to begin a Phase 3 trial for the use of vadadustat in treating anemia in late-stage CKD patients who are not on dialysis. Akebia received feedback from the U.S. Food and Drug Administration (FDA) on its protocol submission for a label expansion study and is incorporating feedback as appropriate. Akebia expects to begin the trial in mid-2025. "We believe Akebia is entering a transformational year with the U.S. market availability of Vafseo, which we believe could become a new standard of care for patients with CKD," said John P. Butler, Chief Executive Officer of Akebia. "During 2025 our commercial organization will remain focused on executing the U.S. launch of Vafseo, while our development team pursues label expansion of Vafseo into the non-dialysis population, which represents a potential multiple billion-dollar market opportunity in the U.S. We believe our commercial products and pipeline have the potential to generate significant shareholder value as Akebia strengthens its leadership position in the treatment of kidney disease and the hypoxia-inducible factor (HIF) space." Vafseo Commercial Update: Vafseo began shipping to dialysis centers and authorized distributors on January 9, 2025. Akebia has secured broad access for Vafseo as the company has now entered into commercial supply agreements with dialysis organizations treating nearly 100% of patients on dialysis in the U.S., including recently signing agreements with a leading dialysis organization and a mid-size dialysis provider. Akebia market research suggests 99% of nephrologists would consider prescribing Vafseo to certain eligible patients, with 75% intending to do so by 6 months after product availability. In December 2024, Akebia announced that U.S. Renal Care enrolled the first patients in the VOICE collaborative clinical trial of Vafseo. U.S. Renal Care has now enrolled more than 650 patients in the trial. Planned Phase 3 Trial of Vadadustat in U.S. Non-Dialysis CKD Patients: In March 2024, the FDA approved Vafseo for the treatment of anemia due to chronic kidney disease in adults who have been receiving dialysis for at least three months. The FDA acknowledged an unmet need for safer and orally available therapies to treat anemia due to CKD in certain non-dialysis patients. Akebia has since engaged with the FDA on potentially expanding vadadustat treatment to this patient population and has received feedback on a protocol submitted for a Phase 3 cardiovascular outcome study of approximately 1,500 U.S. subjects with late-stage CKD anemia not on dialysis, which is expected to begin in mid-2025. Akebia plans to request a Type C meeting with the FDA to continue to discuss the statistical analysis plan and regulatory path. Akebia expects its existing cash resources and cash from operations will be sufficient to fund its current operating plan, including the U.S. Vafseo launch and planned pipeline advancement, for at least two years. Presentation at 43rd J.P. Morgan Healthcare Conference John Butler, Chief Executive Officer, will present on Thursday, January 16th, 2025 at 7:30 a.m. PST. A webcast of the presentation can be accessed through the "Investors" section of Akebia's website for 30 days following the conference. About Akebia Therapeutics Akebia Therapeutics, Inc. is a fully integrated biopharmaceutical company with the purpose to better the lives of people impacted by kidney disease. Akebia was founded in 2007 and is headquartered in Cambridge, Massachusetts. For more information, please visit our website at , which does not form a part of this release. About Vafseo® (vadadustat) tablets Vafseo® (vadadustat) tablets is a once-daily oral hypoxia-inducible factor prolyl hydroxylase inhibitor that activates the physiologic response to hypoxia to stimulate endogenous production of erythropoietin, increasing hemoglobin and red blood cell production to manage anemia. Vafseo is approved for use in 37 countries. INDICATION VAFSEO is indicated for the treatment of anemia due to chronic kidney disease (CKD) in adults who have been receiving dialysis for at least three months. Limitations of Use VAFSEO has not been shown to improve quality of life, fatigue, or patient well-being. VAFSEO is not indicated for use: As a substitute for red blood cell transfusions in patients who require immediate correction of anemia. In patients with anemia due to CKD not on dialysis. IMPORTANT SAFETY INFORMATION about VAFSEO (vadadustat) tablets CONTRAINDICATIONS Known hypersensitivity to VAFSEO or any of its components Uncontrolled hypertension WARNINGS AND PRECAUTIONS Increased Risk of Death, Myocardial Infarction (MI), Stroke, Venous Thromboembolism, and Thrombosis of Vascular Access A rise in hemoglobin (Hb) levels greater than 1 g/dL over 2 weeks can increase these risks. Avoid in patients with a history of MI, cerebrovascular event, or acute coronary syndrome within the 3 months prior to starting VAFSEO. Targeting a Hb level of greater than 11 g/dL is expected to further increase the risk of death and arterial and venous thrombotic events. Use the lowest effective dose to reduce the need for red blood cell (RBC) transfusions. Adhere to dosing and Hb monitoring recommendations to avoid excessive erythropoiesis. Hepatotoxicity Hepatocellular injury attributed to VAFSEO was reported in less than 1% of patients, including one severe case with jaundice. Elevated serum ALT, AST, and bilirubin levels were observed in 1.8%, 1.8%, and 0.3% of CKD patients treated with VAFSEO, respectively. Measure ALT, AST, and bilirubin before treatment and monthly for the first 6 months, then as clinically indicated. Discontinue VAFSEO if ALT or AST is persistently elevated or accompanied by elevated bilirubin. Not recommended in patients with cirrhosis or active, acute liver disease. Hypertension Worsening of hypertension was reported in 14% of VAFSEO and 17% of darbepoetin alfa patients. Serious worsening of hypertension was reported in 2.7% of VAFSEO and 3% of darbepoetin alfa patients. Cases of hypertensive crisis, including hypertensive encephalopathy and seizures, have also been reported in patients receiving VAFSEO. Monitor blood pressure. Adjust anti-hypertensive therapy as needed. Seizures Seizures occurred in 1.6% of VAFSEO and 1.6% of darbepoetin alfa patients. Monitor for new-onset seizures, premonitory symptoms, or change in seizure frequency. Gastrointestinal (GI) Erosion Gastric or esophageal erosions occurred in 6.4% of VAFSEO and 5.3% of darbepoetin alfa patients. Serious GI erosions, including GI bleeding and the need for RBC transfusions, were reported in 3.4% of VAFSEO and 3.3% of darbepoetin alfa patients. Consider this risk in patients at increased risk of GI erosion. Advise patients about signs of erosions and GI bleeding and urge them to seek prompt medical care if present. Serious Adverse Reactions in Patients with Anemia Due to CKD and Not on Dialysis The safety of VAFSEO has not been established for the treatment of anemia due to CKD in adults not on dialysis and its use is not recommended in this setting. In large clinical trials in adults with anemia of CKD who were not on dialysis, an increased risk of mortality, stroke, MI, serious acute kidney injury, serious hepatic injury, and serious GI erosions was observed in patients treated with VAFSEO compared to darbepoetin alfa. Malignancy VAFSEO has not been studied and is not recommended in patients with active malignancies. Malignancies were observed in 2.2% of VAFSEO and 3.0% of darbepoetin alfa patients. No evidence of increased carcinogenicity was observed in animal studies. ADVERSE REACTIONS The most common adverse reactions (occurring at ≥ 10%) were hypertension and diarrhea. DRUG INTERACTIONS Iron supplements and iron-containing phosphate binders: Administer VAFSEO at least 1 hour before products containing iron. Non-iron-containing phosphate binders: Administer VAFSEO at least 1 hour before or 2 hours after non-iron-containing phosphate binders. BCRP substrates: Monitor for signs of substrate adverse reactions and consider dose reduction. Statins: Monitor for statin-related adverse reactions. Limit the daily dose of simvastatin to 20 mg and rosuvastatin to 5 mg. USE IN SPECIFIC POPULATIONS Pregnancy: May cause fetal harm. Lactation: Breastfeeding not recommended until two days after the final dose. Hepatic Impairment : Not recommended in patients with cirrhosis or active, acute liver disease. Please note that this information is not comprehensive. Please click here for the Full Prescribing Information, including BOXED WARNING and Medication Guide. Forward-Looking Statements Statements in this press release regarding Akebia Therapeutics, Inc.'s ("Akebia's") strategy, plans, prospects, expectations, beliefs, intentions and goals are forward-looking statements within the meaning of the U.S. Private Securities Litigation Reform Act of 1995, as amended, and include, but are not limited to, statements regarding: Akebia's plans with respect to its U.S. commercial launch of Vafseo, including Akebia's statements regarding commercial supply contract coverage for Vafseo with dialysis organizations and Akebia's ability to make Vafseo available to nearly 100% of patients on dialysis in the U.S.; Akebia's plans and expectations with respect to potential Vafseo label expansion to treat anemia in late-stage CKD patients who are not on dialysis, including Akebia's expectations as to the timing of a Phase 3 trial, Akebia's statements regarding feedback from the FDA on its protocol submission for a label expansion study and Akebia's plans to request a Type C meeting with the FDA to discuss the statistical plan and regulatory path; Akebia's belief that it is entering a transformational year with U.S. market availability of Vafseo, and Akebia's belief that Vafseo could become a new standard of care for patients with CKD; Akebia's expectations regarding label expansion of Vafseo into the non-dialysis population, including a potential multiple billion-dollar market opportunity in the U.S.; Akebia's belief that its commercial products and pipeline have the potential to generate significant shareholder value as Akebia strengthens its leadership position in the treatment of kidney disease and the HIF space; Akebia's expectations regarding the demand for Vafseo from prescribers; and Akebia's expectations that its existing cash resources and cash from operations will be sufficient to fund its current operating plan, including the U.S. Vafseo launch and planned pipeline advancement, for at least two years. The terms "intend," "believe," "plan," "goal," "potential," "anticipate, "estimate," "expect," "future," "will," "continue," derivatives of these words, and similar references are intended to identify forward-looking statements, although not all forward-looking statements contain these identifying words. Actual results, performance or experience may differ materially from those expressed or implied by any forward-looking statement as a result of various risks, uncertainties and other factors, including, but not limited to, risks associated with: the commercial availability of Vafseo; the potential demand and market potential and acceptance of, as well as coverage and reimbursement related to, Auryxia® and Vafseo, including estimates regarding the potential market opportunity; the competitive landscape for Auryxia and Vafseo, including potential generic entrants; the ability of Akebia to attract and retain qualified personnel; Akebia's ability to implement cost avoidance measures and reduce operating expenses; decisions made by health authorities, such as the FDA, with respect to regulatory filings and other interactions; the potential therapeutic benefits, safety profile, and effectiveness of Vafseo; the results of preclinical and clinical research; manufacturing, supply chain and quality matters and any recalls, write-downs, impairments or other related consequences or potential consequences; and early termination of any of Akebia's collaborations. Other risks and uncertainties include those identified under the heading "Risk Factors" in Akebia's Quarterly Report on Form 10-Q for the quarter ended September 30, 2024, and other filings that Akebia may make with the U.S. Securities and Exchange Commission in the future. These forward-looking statements (except as otherwise noted) speak only as of the date of this press release, and, except as required by law, Akebia does not undertake, and specifically disclaims, any obligation to update any forward-looking statements contained in this press release. Akebia Therapeutics®, Auryxia and Vafseo® are registered trademarks of Akebia Therapeutics, Inc. and its affiliates. Akebia Therapeutics Contact Mercedes Carrasco [email protected] SOURCE Akebia Therapeutics, Inc. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Phase 3Drug ApprovalClinical Result

12 Dec 2024

·www.businesswire.com

Corcept Announces Positive Results in Treatment Phase of CATALYST Trial in Patients With Hypercortisolism (Cushing’s Syndrome) and Difficult-to-Control Diabetes

REDWOOD CITY, Calif.--( BUSINESS WIRE )--Corcept Therapeutics Incorporated (NASDAQ: CORT), a commercial-stage company engaged in the discovery and development of medications to treat severe endocrinologic, oncologic, metabolic and neurologic disorders by modulating the effects of the hormone cortisol, today announced that the primary endpoint was met in the treatment phase of CATALYST, a randomized, double-blind, placebo-controlled study of Korlym ® in patients with hypercortisolism (Cushing’s syndrome) and difficult-to-control type 2 diabetes. CATALYST is a prospective, Phase 4 study with two parts. The first part assessed the prevalence of hypercortisolism by screening 1057 patients with difficult-to-control type 2 diabetes, defined as hemoglobin A1c greater than 7.5 percent despite receiving optimal therapies, including GLP-1 agonists. Of these patients, 23.8 percent were identified as having hypercortisolism and were eligible to enter CATALYST’s treatment phase, in which 136 patients were randomized, 2:1, to receive either Korlym or placebo for 24 weeks. The primary endpoint was the reduction in hemoglobin A1c between these groups. CATALYST met its primary endpoint. Patients who received Korlym exhibited a clinically meaningful and statistically significant improvement in hemoglobin A1c, with a decrease from baseline of 1.47 percent as compared to a decrease of 0.15 percent in patients who received placebo (placebo-adjusted reduction of 1.32 percent; p-value: < 0.0001). The safety profile of Korlym in this study was consistent with the medication’s label and no new side effects or adverse events were identified. Complete results from CATALYST will be presented at a medical conference next year. “CATALYST’s first part showed that hypercortisolism is much more common than previously assumed. The results announced today show that Korlym is a safe and effective treatment option,” said Ralph DeFronzo, MD, chief of the Diabetes Division and professor of medicine at UT Health San Antonio and CATALYST study investigator. “Reductions in hemoglobin A1c of this magnitude are of great clinical benefit. They are particularly compelling, given that the patients in CATALYST had been receiving our best therapies – but continued to experience serious disease. These findings should prompt expanded screening for hypercortisolism, more effective treatment and better health outcomes for patients who are struggling today.” “The results of the CATALYST study will enable physicians to more accurately diagnose and treat patients with hypercortisolism - a serious and deadly disease,” said Bill Guyer, PharmD, Corcept’s Chief Development Officer. “One in four patients with difficult-to-control type 2 diabetes have hypercortisolism and Korlym, a cortisol modulator, was highly effective in controlling hyperglycemia in this patient population.” About Hypercortisolism (Cushing’s Syndrome) Hypercortisolism is caused by excessive activity of the hormone cortisol. Symptoms vary, but most patients experience one or more of the following manifestations: hypertension, central obesity, elevated blood sugar and difficult-to-control type 2 diabetes, severe fatigue and weak muscles. Irritability, anxiety, depression and cognitive disturbances are common. Hypercortisolism can affect every organ system and can be lethal if not treated effectively. Important information about Korlym follows, and full Prescribing Information, including BOXED WARNING , and a Medication Guide are available at www.korlym.com . IMPORTANT SAFETY INFORMATION INDICATIONS AND USAGE Korlym (mifepristone) is a cortisol receptor blocker indicated to control hyperglycemia secondary to hypercortisolism in adult patients with endogenous Cushing’s syndrome who have type 2 diabetes mellitus or glucose intolerance and have failed surgery or are not candidates for surgery. IMPORTANT LIMITATIONS OF USE Do not use for the treatment of type 2 diabetes mellitus unrelated to endogenous Cushing’s syndrome. BOXED WARNING: TERMINATION OF PREGNANCY Mifepristone is a potent antagonist of progesterone and cortisol via the progesterone and glucocorticoid (GR-II) receptors, respectively. The antiprogestational effects will result in the termination of pregnancy. Pregnancy must therefore be excluded before the initiation of treatment with Korlym and prevented during treatment and for one month after stopping treatment by the use of a nonhormonal medically acceptable method of contraception unless the patient has had a surgical sterilization, in which case no additional contraception is needed. Pregnancy must also be excluded if treatment is interrupted for more than 14 days in females of reproductive potential. DOSAGE AND ADMINISTRATION Obtain a negative pregnancy test prior to initiating treatment with Korlym in females of reproductive potential, or if treatment is interrupted for more than 14 days. Administer once daily orally with a meal. The recommended starting dose is 300 mg once daily. Renal impairment: Do not exceed 600 mg once daily. Mild-to-moderate hepatic impairment: Do not exceed 600 mg once daily. Do not use in severe hepatic impairment. Based on clinical response and tolerability, the dose may be increased in 300-mg increments to a maximum of 1200 mg once daily. Do not exceed 20 mg/kg per day. Concomitant use of Korlym with a strong CYP3A inhibitor resulted in a 38% increase in mean plasma concentration of mifepristone. For patients already being treated with a strong CYP3A inhibitor, start with a Korlym dose of 300 mg per day and titrate to a maximum of 900 mg per day if clinically indicated. When a strong CYP3A inhibitor is administered to patients already receiving Korlym, adjust the dose as follows: for patients receiving a daily dose of 600 mg, reduce dose to 300 mg. For patients receiving a daily dose of 900 mg, reduce dose to 600 mg. For patients receiving a daily dose of 1200 mg, reduce dose to 900 mg. Titrate if clinically indicated and do not exceed a Korlym dose of 900 mg in combination with a strong CYP3A inhibitor. CONTRAINDICATIONS Pregnancy; patients taking simvastatin or lovastatin and CYP3A substrates with narrow therapeutic ranges; patients receiving systemic corticosteroids for lifesaving purposes; women with a history of unexplained vaginal bleeding or endometrial hyperplasia with atypia or endometrial carcinoma; patients with known hypersensitivity to mifepristone or to any of the product components. WARNINGS AND PRECAUTIONS Adrenal insufficiency: Patients should be closely monitored for signs and symptoms of adrenal insufficiency. Hypokalemia: Hypokalemia should be corrected prior to treatment and monitored for during treatment. Vaginal bleeding and endometrial changes: Women may experience endometrial thickening or unexpected vaginal bleeding. Use with caution if the patient also has a hemorrhagic disorder or is on anticoagulant therapy. QT interval prolongation: Avoid use with QT interval-prolonging drugs, or in patients with potassium channel variants resulting in a long QT interval. Use of strong CYP3A inhibitors: Concomitant use increases mifepristone plasma levels. Adjust Korlym dose as described in Dosage and Administration . Use only when necessary and do not exceed a Korlym dose of 900 mg. ADVERSE REACTIONS Most common adverse reactions in Cushing’s syndrome (≥20%): nausea, fatigue, headache, decreased blood potassium, arthralgia, vomiting, peripheral edema, hypertension, dizziness, decreased appetite, endometrial hypertrophy. DRUG INTERACTIONS Drugs metabolized by CYP3A: Administer drugs that are metabolized by CYP3A at the lowest dose when used with Korlym. CYP3A inhibitors: Caution should be used when Korlym is used with strong CYP3A inhibitors. Adjust Korlym dose as described in Dosage and Administration . Use only when necessary, and do not exceed a Korlym dose of 900 mg. CYP3A inducers: Do not use Korlym with CYP3A inducers. Drugs metabolized by CYP2C8/2C9: Use the lowest dose of CYP2C8/2C9 substrates when used with Korlym. Drugs metabolized by CYP2B6: Use of Korlym should be done with caution with bupropion and efavirenz. Hormonal contraceptives: Do not use with Korlym. USE IN SPECIFIC POPULATIONS Lactation: Mifepristone is present in human milk, however, there are no data on the amount of mifepristone in human milk, the effects on the breastfed infant, or the effects on milk production during long term use of mifepristone. About Corcept Therapeutics For over 25 years, Corcept’s focus on cortisol modulation and its potential to treat patients with a wide variety of serious disorders has led to the discovery of more than 1,000 proprietary selective cortisol modulators. Corcept is conducting advanced clinical trials in patients with hypercortisolism, solid tumors, ALS and liver disease. In February 2012, the company introduced Korlym, the first medication approved by the U.S. Food and Drug Administration for the treatment of patients with endogenous hypercortisolism. Corcept is headquartered in Redwood City, California. For more information, visit Corcept.com. Forward-Looking Statements Statements in this press release, other than statements of historical fact, are forward-looking statements based on our current plans and expectations and are subject to risks and uncertainties that might cause our actual results to differ materially from those such statements express or imply. These risks and uncertainties are set forth in our SEC filings, which are available at our website and the SEC’s website. In this press release, forward-looking statements include those concerning the full results of CATALYST and the date and manner of their publication; changes in medical practice, including in the frequency and clinical outcome of screening patients for hypercortisolism; the adoption of Korlym as a treatment for patients with hypercortisolism and difficult-to-control diabetes; and Korlym’s commercial prospects. We disclaim any intention or duty to update forward-looking statements made in this press release.

Clinical ResultPhase 3Drug ApprovalPhase 2

11 Dec 2024

·www.echemi.com

Heng Rui Pharma Launches Phase III Trial for ANGPTL3 Monoclonal Antibody

According to information from the U.S. clinical trial registry Clinicaltrials on December 10, Chinese company Heng Rui Pharma has launched its first Phase III clinical trial (SHR-1918-301) for the ANGPTL3 monoclonal antibody SHR-1918. This drug marks the first domestic ANGPTL3 monoclonal antibody to enter the Phase III clinical trial stage. SHR-1918 is an ANGPTL3 monoclonal antibody developed by Heng Rui Pharma, which works by inhibiting ANGPTL3 activity to lower triglycerides (TG) and low-density lipoprotein cholesterol (LDL-C) levels in serum. LDL-C and TG are significant risk factors for the development of atherosclerotic cardiovascular diseases. ANGPTL3 plays a key role in lipid metabolism regulation by inhibiting lipoprotein lipase and endothelial lipase, thereby reducing the clearance of TG and LDL-C. In September this year, Heng Rui Pharma announced the results of its first Phase I study (SHR-1918-101) at the European Society of Cardiology (ESC) annual meeting. The study showed that SHR-1918 (100-1200mg, subcutaneously) demonstrated good tolerance and pharmacokinetic characteristics in healthy subjects, with a peak time of 8.0-10.0 days and a half-life of 29.4-53.5 days. Additionally, SHR-1918 effectively and durably reduced LDL-C and TG levels: patients receiving doses of SHR-1918 of 300mg or higher had LDL-C levels reduced by over 30% (up to 49.1%), lasting more than 64 days; TG levels were reduced by over 50% (up to 82.8%), lasting more than 85 days. Given the potential of SHR-1918 for treating rare dyslipidemia disorders, the drug received breakthrough therapy designation for homozygous familial hypercholesterolemia (HoFH) from the Chinese National Medical Products Administration (NMPA) in September. The launched Phase III study is a multicenter, randomized, double-blind, placebo-controlled clinical trial (n=45), aimed at evaluating the efficacy and safety of SHR-1918 in treating homozygous familial hypercholesterolemia (HoFH). The primary endpoint is the percentage change in LDL-C levels from baseline at week 12. Homozygous familial hypercholesterolemia (HoFH) is a rare and severe genetic disorder where patients accumulate LDL-C in the blood due to defects or deficiencies in low-density lipoprotein receptors (LDLR), increasing the risk of heart disease and stroke. Currently, available treatment options for these patients include statins (simvastatin, atorvastatin, and rosuvastatin), ezetimibe, lomitapide, mipomersen, PCSK9 monoclonal antibodies (evolocumab and alirocumab), and evinacumab. Among these, evinacumab (Regeneron/Ultragenyx) is the only marketed ANGPTL3 monoclonal antibody, with global sales of $80.9 million in 2023.

Phase 3Clinical ResultPhase 1Breakthrough TherapyPhase 2

100 Deals associated with Simvastatin

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KEGG	Wiki	ATC	Drug Bank
D00434	Simvastatin	C10AA01	DB00641

R&D Status

Approved

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Indication	Country/Location	Organization	Date
Hyperlipoproteinemia Type V	CN	Hangzhou MSD Pharmaceutical Co. Ltd.	01 Jan 1997
Coronary Disease	US	Organon & Co.	23 Dec 1991
Hyperlipidemias	JP	Organon & Co.	04 Oct 1991
Hyperlipoproteinemia Type II	JP	Organon & Co.	04 Oct 1991
Coronary Artery Disease	AU	Organon Pharma Pty Ltd.	12 Sep 1991
Heterozygous familial hypercholesterolemia	AU	Organon Pharma Pty Ltd.	12 Sep 1991
Hypercholesterolemia	AU	Organon Pharma Pty Ltd.	12 Sep 1991
Stroke	AU	Organon Pharma Pty Ltd.	12 Sep 1991

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Primary hypercholesterolemia	Phase 3	-	Merck Sharp & Dohme Corp.	01 Jul 2007
Hyperlipidemia, Familial Combined	Phase 3	-	Merck Sharp & Dohme Corp.	24 Jan 2006
Combined hyperlipidemia	Phase 3	-	Organon & Co.	01 May 2002
Diabetes Mellitus, Type 2	Phase 3	-	Organon & Co.	01 Dec 2001
Homozygous familial hypercholesterolemia	Phase 3	-	Organon & Co.	03 May 2000
Acute Coronary Syndrome	Phase 3	-	Organon & Co.	01 Nov 1999
Chest Pain	Phase 3	-	Organon & Co.	01 Nov 1999
Myocardial Infarction	Phase 3	-	Organon & Co.	01 Nov 1999
Cardiovascular Diseases	Phase 3	GB	Merck Sharp & Dohme Corp.	01 Jul 1998
Carotid Artery Diseases	Phase 2	-	Merck Sharp & Dohme Corp.	01 Apr 2009

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ACTRN12617001087347 (ASCO_GI2025)	Phase 2	Rectal Cancer Neoadjuvant	135	Simvastatin 40mg	cvmlvhhonq(pvonylrifh) = jfndcfeppc mgpiurwteu (mykhkhbkmj ) View more	Positive	23 Jan 2025
				Placebo	cvmlvhhonq(pvonylrifh) = pnshvwwlgt mgpiurwteu (mykhkhbkmj ) View more
ISRCTN12940165 (Pubmed \| Clin Exp Dent Res) Manual	Not Applicable	Dental Pulp Necrosis	38	modified 3Mix-Simvastatin combinationSimvastatinix-Simvastatin combination (Conventional pulpectomy)	ikyqogantp(izgsydsnwf) = xxxxlilzum imdgkhtwyq (texgqsvqqv )	Positive	01 Apr 2024
				Non-instrumentation endodontic treatment (NIET) using 3Mixtatin	ikyqogantp(izgsydsnwf) = zirhrldprg imdgkhtwyq (texgqsvqqv )
NCT04638400 (CTgov)	Phase 4	Inflammation \| Atherosclerosis \| Obesity ... View more	10	Simvastatin 40mg (Simvastatin)	edpfacqfzu(tqincmghnf) = topcnrobun rmpbbkhcbu (ubxlfegjgn, vddkjgekxe - advevqtjxg) View more	-	23 Jan 2024
				Ezetimibe 10mg (Ezetimibe)	edpfacqfzu(tqincmghnf) = vvnelnxfjz rmpbbkhcbu (ubxlfegjgn, pmtlsqvlxu - ymcvyhgmmk) View more
NCT02735707 (REMAP-CAP, Pubmed \| N Engl J Med)	Phase 3	COVID-19	2,684	Simvastatin 80 mg daily	cwyaueoqjr(qavvetccni) = rmiacibugx tiufumcfku (eoktapzrhs, 0.95 - 1.32)	Negative	21 Dec 2023
NCT04514029 (ASH2023)	Early Phase 1	Carney Complex	15	Simvastatin 40 mg + Intrathecal Dexamethasone	venyziqjnb(dzxttvkelc) = ucteqkwbjp axkrwlocpb (wztogcpzsi )	-	10 Dec 2023
NCT00988364 (Merck-123, CTgov)	Phase 4	Metabolic Syndrome	30	ezetimibe (Ezetimibe)	hyvzxljdmu(kinythsiwl) = ehwscdmomk utfozvctfu (sbsdtoxddi, qpqcqkdwva - pkyzehqqtj) View more	-	30 Nov 2023
				Simvastatin (Simvastatin)	hyvzxljdmu(kinythsiwl) = suposcwcyo utfozvctfu (sbsdtoxddi, dbttqtnost - vcmibeblpo) View more
NCT03454529 (CTgov)	Phase 2	Invasive Mammary Carcinoma \| Early Stage Breast Carcinoma	24	Laboratory Biomarker Analysis+Simvastatin	iuxwdhiuhv(xajdvcfkji) = kgjtctjmkw tiiflkxjsm (pkooklrxhn, sfmifpqnlu - mcgmzuahie) View more	-	01 Aug 2023
NCT04507373 (CTgov)	Phase 4	Pain \| Drug-Related Side Effects and Adverse Reactions \| Muscle Weakness ... View more	3	Simvastatin 40mg (Placebo)	ofbzhilcod(jhoqnatdto) = qaewmousry wjscodgpwl (vbluafjkea, gyhxltatbw - rwxygcudkg) View more	-	14 Feb 2023
				Simvastatin 40mg (Simvastatin 40mg)	ofbzhilcod(jhoqnatdto) = ralwvxrjbe wjscodgpwl (vbluafjkea, vddmaatros - mtmbfxnkmd) View more
NCT03452891 (CTgov)	Phase 4	Periodontal Diseases	50	Methylcellulose	cofbwktvji(cwklprekrl) = quppzwtsqw lmkloqkrmp (qzxnuorzsp, awmwcrevkb - yxkedrruxv) View more	-	09 Feb 2023
AAIC2022	Not Applicable	Alzheimer Disease	-	Simvastatin loaded SNEDDS	neyvbkxvwo(wwsrzbjgtk) = fkotgoxqps bnvivbuvcq (pjasgcnnjh )	-	20 Dec 2022

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