Sintbilo (tafolecimab) / Innovent Biologics - LARVOL DELTA

TAFOLECIMAB IN CHINESE PATIENTS WITH DIABETES MELLITUS: A POOLED ANALYSIS OF EFFICACY AND SAFETY DATA FROM PHASE 3 RANDOMIZED, PLACEBO-CONTROLLED TRIALS - Hua Shen (ACC 2025) - "In Chinese patients with diabetes mellitus, tafolecimab 450 mg Q4W yields promising lipid-lowering efficacy and is generally well-tolerated."

P3 data • Retrospective data • Diabetes • Dyslipidemia • Metabolic Disorders • APOB

Cost-Effectiveness and Price Threshold Analysis of Tafolecimab in Chinese Patients with Elevated LDL Cholesterol Despite Statin Therapy. (PubMed, Am J Cardiovasc Drugs) - "From the perspective of the Chinese healthcare system, the cost-effective annual price threshold for tafolecimab for patients with hypercholesterolemia was CNY 7022, at a threshold of CNY 268,074 per QALY."

HEOR • Journal • Cardiovascular • Dyslipidemia • Metabolic Disorders • Myocardial Infarction

Tafolecimab, a Third Monoclonal Antibody for PCSK9 as the Novel Lipid-Lowering Drug Around the World: A Narrative Review. (PubMed, Drugs) - "The long-acting formulation of tafolecimab enables less frequent dosing, thereby promoting compliance. As cardiovascular diseases continue to escalate globally, tafolecimab holds promise not only for patients in China but also for broader international applications, representing a critical advancement in the evolving landscape of lipid-lowering therapies."

Journal • Review • Atherosclerosis • Cardiovascular • Dyslipidemia • Metabolic Disorders • APOB

The clinical efficacy of PCSK9 inhibitors in neoadjuvant concurrent chemoradiotherapy combined with PD-1 inhibitors in the treatment of gastrointestinal malignancies: a prospective multicenter randomized controlled clinical trial (ChiCTR) - P1 | N=110 | Sponsor: The First Hospital of Lanzhou University; The First Hospital of Lanzhou University

New P1 trial • Cardiovascular • Gastrointestinal Cancer • Gastrointestinal Disorder • Oncology

PCSK9 Inhibitors for ASCVD Risk Reduction in Asian Populations — a meta-analysis of efficacy and safety profiles (AHA 2024) - "Inclisiran was used in 3 studies, evolocumab in 5, alirocumab in 2, and tafolecimab in 1, alongside statins or ezetimibe.PCSK9i reduced LDL by -74.21 mg/dL and increased the likelihood of >50% LDL reduction compared to placebo (RR: 37.41, 95% CI: 16.31-85.82, P < 0.00001; I^2: 0%). The considerable heterogeneity in LDL reduction may result from variations in dosing, different agents used, baseline LDL levels, and geographical diversity. Future research should explore effects across more ethnicities to enhance generalizability."

Retrospective data • Dyslipidemia • Metabolic Disorders

Proprotein Convertase Subtilisin/Kexin Type 9 Inhibitors and Lipid Reduction: A Network Meta-Analysis (AHA 2024) - "In patients with hypercholesterolemia and/or hyperlipidemia treated with medium-intensity statins, tafolecimab and evolocumab (either Q2W or Q4W) might be preferred choices for lowering LDL-C. Additionally, tafolecimab (either Q2W or Q4W) appears to be the most effective agent for reducing lipoprotein(a) levels."

Retrospective data • Dyslipidemia • Metabolic Disorders

Innovent Announces First-Time Inclusion of SINTBILO...in China's National Reimbursement Drug List (PRNewswire) - "In the updated NRDL, SINTBILO is newly listed for the treatment of adult patients with primary hypercholesterolemia (including heterozygous familial and non-familial types) and mixed dyslipidemia. SINTBILO (tafolecimab injection) is Innovent's first entry into the cardiovascular field, offering multiple dosing options: 150mg Q2W, 450mg Q4W, and 600mg Q6W. These regimens significantly reduce low-density lipoprotein cholesterol (LDL-C) levels by nearly 70% and lower lipoprotein a [Lp(a)] by nearly 50%. As the first domestic PCSK9 inhibitor in the NRDL, SINTBILO provides an important new treatment option for cholesterol management in China, improving quality of life for a broad population of patients with hypercholesterolemia."

Reimbursement • Dyslipidemia • Heterozygous Familial Hypercholesterolemia

IMPROVE-AMI: Effectiveness of Proprotein Convertase Subtilisin/kexin Type 9 (PCSK9) Inhibitor Initiation Before Percutaneous Coronary Intervention on Acute Myocardial Infarction Patients (clinicaltrials.gov) - P4 | N=1160 | Not yet recruiting | Sponsor: The Affiliated Hospital of Xuzhou Medical University

New P4 trial • Cardiovascular • Myocardial Infarction

A Study of IBI306 in Participants With Hypercholesterolemia (clinicaltrials.gov) - P3 | N=306 | Completed | Sponsor: Innovent Biologics (Suzhou) Co. Ltd. | Recruiting ➔ Completed

Trial completion • Dyslipidemia • Metabolic Disorders

The efficacy and safety of proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors combined with statins in patients with hypercholesterolemia: a network meta-analysis. (PubMed, Front Cardiovasc Med) - "Notably, evolocumab exhibited the most pronounced effect with a treatment difference of -63.67% (-68.47% to -58.87%) compared with placebo...Furthermore, the safety profile of PCSK9 inhibitors was favorable with no increase in the incidence of AE, SAE, or AE leading to treatment discontinuation; however, alirocumab, inclisiran, and tafolecimab may potentially entail a potential risk associated with injection-site reactions...Furthermore, PCSK9 inhibitors and ezetimibe exhibit similar safety profiles. [PROSPERO], identifier [CRD42023490506]."

Journal • Retrospective data • Review • Dyslipidemia • Metabolic Disorders • APOB

Antibodies to watch in 2024. (PubMed, MAbs) - "In this installment, we discuss key details for 16 antibody therapeutics granted a first approval in 2023, as of November 17 (lecanemab (Leqembi), rozanolixizumab (RYSTIGGO), pozelimab (VEOPOZ), mirikizumab (Omvoh), talquetamab (Talvey), elranatamab (Elrexfio), epcoritamab (EPKINLY), glofitamab (COLUMVI), retifanlimab (Zynyz), concizumab (Alhemo), lebrikizumab (EBGLYSS), tafolecimab (SINTBILO), narlumosbart (Jinlitai), zuberitamab (Enrexib), adebrelimab (Arelili), and divozilimab (Ivlizi))...These nearly 50 product candidates include numerous innovative bispecific antibodies, such as odronextamab, ivonescimab, linvoseltamab, zenocutuzumab, and erfonrilimab, and antibody-drug conjugates, such as trastuzumab botidotin, patritumab deruxtecan, datopotamab deruxtecan, and MRG002, as well as a mixture of two immunocytokines (bifikafusp alfa and onfekafusp alfa)...Our analyses indicate that these molecules have approval success rates in the range of 14-32%, with higher rates..."

Journal • Infectious Disease • Novel Coronavirus Disease • Oncology • Respiratory Diseases

The efficacy and safety of chemotherapy with Tafolecimab and Sintilimab in advanced or metastatic driver-gene-negative non-small cell lung cancer after first-line immunotherapy failure: a prospective, single arm phase II clinical study.tive non-small cell lung cancer patients after first-line immunotherapy failure (ChiCTR) - P2 | N=30 | Not yet recruiting | Sponsor: Beijing Chest Hospital, Capital Medical University; Beijing Chest Hospital, Capital Medical University

IO biomarker • Metastases • New P2 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ALK • EGFR • PD-L1

The Efficacy of Tafolecimab in Chinese Patients with Hypercholesterolemia: A Systematic Review and Meta-analysis. (PubMed, Am J Cardiovasc Drugs) - "Tafolecimab showed promising lipid-lowering efficacy and a well-tolerated safety profile. Our findings suggest its potential as an innovative therapeutic option for individuals with hypercholesterolemia; however, significant heterogeneity was observed in some results, making it difficult to come to a firm conclusion. Therefore, large-scale randomized trials are required to confirm our findings, particularly exploring the most effective dosage regimens across varied populations."

Journal • Retrospective data • Review • Atherosclerosis • Cardiovascular • Dyslipidemia • Metabolic Disorders • APOB

A Prospective, Single-arm, Phase II Clinical Trial to Evaluate the Efficacy and Safety of Tafolecimab and Sintilimab Combined With Chemotherapy in Patients With Advanced or Metastatic Driver Gene-negative Non-small Cell Lung Cancer After Failure of First-line Immunotherapy. (clinicaltrials.gov) - P2 | N=30 | Recruiting | Sponsor: Jinghui Wang

IO biomarker • Metastases • New P2 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • PD-L1

Hypercholesterolemia: a literature review on management using tafolecimab: a novel member of PCSK9 monoclonal antibodies. (PubMed, Ann Med Surg (Lond)) - "Hyperlipidemia management includes various lipid-lowering drugs, including statins, Bempedoic acid, inclisiran, Lomitapide, ANGPTL3 inhibitors, and PCSK9 inhibitors...It has also been found that Tafolecimab has more affinity for PCSK9 and a longer duration of LDL-C reduction than other monoclonal antibody drugs such as evolocumab...Regulatory authorities like the FDA and EMA should also evaluate Tafolecimab's risks and benefits. In conclusion, Tafolecimab shows potential as an innovative therapeutic option for hypercholesterolaemia, particularly in patients with specific risk factors, but warrants additional research."

Journal • Review • Atherosclerosis • Cardiovascular • Dyslipidemia • Metabolic Disorders • ANGPTL3

Network Meta-Analysis to Compare the Efficacy Between Different Classes of PCSK9 Inhibitors, siRNA Vs. PCSK9 mAb, in Asian Patients With Hypercholesterolemia at Increased Cardiovascular Risk (ISPOR 2024) - "This NMA ascertains that in Asian patients with hypercholesterolemia, at increased CV risk and at MTDS, inclisiran (siRNA) with twice-yearly dosing is expected to show clinically meaningful LDL-C reductions comparable to PCSK9i mAb."

Retrospective data • Cardiovascular • Dyslipidemia • Metabolic Disorders

Targeting proprotein convertase subtilisin/kexin type 9 (PCSK9): from bench to bedside. (PubMed, Signal Transduct Target Ther) - "The advent and clinical approval of innovative PCSK9 inhibitory therapies (PCSK9-iTs), including three monoclonal antibodies (Evolocumab, Alirocumab, and Tafolecimab) and one small interfering RNA (siRNA, Inclisiran), have marked a significant breakthrough in cardiovascular medicine. In conclusion, this synthesized review integrates existing knowledge and novel insights on PCSK9, providing a holistic perspective on its transformative impact in reshaping therapeutic paradigms across various disorders. It emphasizes the clinical value and effect of PCSK9-iT, underscoring its potential in advancing the landscape of biomedical research and its capabilities in heralding new eras in personalized medicine."

Journal • Review • Cardiovascular • Dyslipidemia • Hepatology • Immunology • Infectious Disease • Metabolic Disorders • Oncology • PCSK9

Multiple Ascending Dose Study of PCSK-9 Inhibitor (IBI306) in Chinese Patients With Hypercholesterolemia (clinicaltrials.gov) - P2 | N=60 | Completed | Sponsor: Innovent Biologics (Suzhou) Co. Ltd. | Unknown status ➔ Completed

Trial completion • Dyslipidemia • Metabolic Disorders

Tafolecimab: First Approval. (PubMed, Drugs) - "Tafolecimab was approved in August 2023 in China as an adjunct to diet, in combination with a statin or statin with other low-density lipoprotein cholesterol (LDL-C)-lowering therapies, for the treatment of adults with primary hyperlipidemia [including heterozygous familial hypercholesterolemia (HeFH) and non-familial hypercholesterolemia (non-FH)] and mixed dyslipidemia who have failed to achieve LDL-C goals despite moderate or higher doses of statins, to reduce LDL-C, total cholesterol (TC), and apolipoprotein B (ApoB) levels. This article summarizes the milestones in the development of tafolecimab leading to this first approval for the treatment of adults with primary hyperlipidemia and mixed dyslipidemia."

Journal • Review • Dyslipidemia • Genetic Disorders • Heterozygous Familial Hypercholesterolemia • Metabolic Disorders • APOB

Pharmacokinetic/LDL-C and Exposure-Response Analysis of Tafolecimab in Chinese Hypercholesterolemia Patients: Results from Phase 1, 2 and 3 studies. (PubMed, Clin Transl Sci) - "There was no exposure dependency observed in exposure-safety exploration. The PopPK/LDL-C model was successfully developed, validated, and predicted tafolecimab/LDL-C concentrations and individual exposures."

Journal • PK/PD data • Dyslipidemia • Metabolic Disorders

Early Initiation of Tafolecimab for Patients With Acute Coronary Syndromeundergoing Percutaneous Coronary Intervention in Chinese Population (clinicaltrials.gov) - P=N/A | N=3684 | Not yet recruiting | Sponsor: China National Center for Cardiovascular Diseases

New trial • Acute Coronary Syndrome • Cardiovascular

Tafolecimab in Chinese patients with non-familial hypercholesterolemia (CREDIT-1): a 48-week randomized, double-blind, placebo-controlled phase 3 trial. (PubMed, Lancet Reg Health West Pac) - "Tafolecimab dosed at 450 mg Q4W and 600 mg Q6W was safe and showed superior lipid-lowering efficacy versus placebo, providing a novel treatment option for Chinese hypercholesterolemia patients. This study was sponsored by Innovent Biologics, Inc."

Clinical • Journal • P3 data • Cardiovascular • Dyslipidemia • Genetic Disorders • Infectious Disease • Metabolic Disorders • Nephrology • Respiratory Diseases • APOB

Bioequivalence Study of Tafolecimab Injections in Chinese Healthy Male Volunteers (clinicaltrials.gov) - P1 | N=166 | Completed | Sponsor: Innovent Biologics (Suzhou) Co. Ltd. | Active, not recruiting ➔ Completed

Trial completion

Tafolecimab, A Novel Member of PCSK9 Monoclonal Antibodies, Is Worth Expecting in a Chinese Population. (PubMed, JACC Asia) - No abstract available

Journal • Cardiovascular • Coronary Artery Disease • Dyslipidemia • Metabolic Disorders

Tafolecimab in Chinese Patients With Hypercholesterolemia (CREDIT-4): A Randomized, Double-Blind, Placebo-Controlled Phase 3 Trial. (PubMed, JACC Asia) - P3 | "Tafolecimab was safe and showed robust lipid-lowering efficacy in Chinese patients at high or very high cardiovascular risk with hypercholesterolemia. (A Study of IBI306 in Participants With Hypercholesterolemia; NCT04709536)."

Clinical • Journal • P3 data • Cardiovascular • Coronary Artery Disease • Dyslipidemia • Genetic Disorders • Heterozygous Familial Hypercholesterolemia • Infectious Disease • Metabolic Disorders • Nephrology • APOB