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Article ; Online: Human Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of ASC42, a Novel Farnesoid X Receptor Agonist.

He, Handan / Wu, Jinzi J

2023 Volume 23, Issue 4, Page(s) 453–464

Abstract: Background: ASC42 is a non-steroidal farnesoid X receptor agonist currently in clinical development for chronic liver diseases, such as nonalcoholic fatty liver disease/nonalcoholic steatohepatitis (NAFLD/NASH) and primary biliary cirrhosis (PBC).: ... ...

Abstract	Background: ASC42 is a non-steroidal farnesoid X receptor agonist currently in clinical development for chronic liver diseases, such as nonalcoholic fatty liver disease/nonalcoholic steatohepatitis (NAFLD/NASH) and primary biliary cirrhosis (PBC). Objective: The objective of this study was to assess the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of ASC42 in healthy subjects. Methods: We conducted the first-in-human study of ASC42 following single and multiple ascending doses (SAD/MAD) and food effect in healthy subjects. The SAD study included five cohorts receiving 5-200 mg ASC42 or placebo and one cohort that was given 15 mg ASC42 with a high-fat meal. The MAD study included three cohorts receiving 5-50 mg ASC42 or placebo once-daily (QD) for 14 days. Results: A total of 65 healthy subjects were enrolled and one subject in the MAD study (cohort 8, ASC42 50 mg) withdrew from the study due to an unrelated serious adverse event (SAE) of atrial fibrillation. Pruritus was observed at the highest doses (200 mg cohort in SAD and 50 mg cohort in MAD). Most AEs were mild or moderate. No life-threatening or fatal AEs occurred. ASC42 showed a proportional increase in exposure and elimination half-life following both single and multiple dosing. There was a 21% and 37% decrease in area under the curve (AUC) and maximum plasma concentration (C Conclusion: ASC42 was well tolerated with a pharmacokinetic profile suitable for QD dosing, and demonstrated dose-dependent targets engagement without altering plasma cholesterol in healthy subjects. Trial registration number: NCT04679129.
MeSH term(s)	Humans ; Dose-Response Relationship, Drug ; Double-Blind Method ; Area Under Curve ; Healthy Volunteers ; Cholesterol
Chemical Substances	Cholesterol (97C5T2UQ7J)
Language	English
Publishing date	2023-11-02
Publishing country	New Zealand
Document type	Journal Article
ZDB-ID	2020476-0
ISSN	1179-6901 ; 1174-5886
ISSN (online)	1179-6901
ISSN	1174-5886
DOI	10.1007/s40268-023-00444-4
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Book ; Online: Long-term positive severe acute respiratory syndrome coronavirus 2 ribonucleic acid and therapeutic effect of antivirals in patients with coronavirus disease

Wei, Bo / Hang, Xiaofeng / Xie, Ying / Zhang, Yuanjing / Wang, Jianrong / Cao, Xinghao / Wu, Jinzi J. / Wang, Junxue

Revista da Sociedade Brasileira de Medicina Tropical v.53 2020

Case reports

2020

Abstract: Abstract Coronavirus disease (COVID-19), caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has been declared a pandemic. We herein report four COVID-19 cases with long-term positive viral ribonucleic acid (RNA) for about 61 days. ...

Abstract	Abstract Coronavirus disease (COVID-19), caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has been declared a pandemic. We herein report four COVID-19 cases with long-term positive viral ribonucleic acid (RNA) for about 61 days. Despite treatment with recombinant human interferon, convalescent plasma from COVID-19 patients, arbidol, etc., nucleic acid results were still positive for SARS-CoV-2. After treatment with ritonavir-boosted danoprevir (DNVr, 100/100 mg, once daily), all four patients showed two to three consecutive negative SARS-CoV-2 RNA and were thus discharged from hospital. Therefore, DNVr may be a potentially effective antiviral for COVID-19 patients with long-term positive SARS-CoV-2 RNA.
Keywords	COVID-19 ; Antivirals ; Long-term positive SARS-CoV-2 ; covid19
Language	English
Publishing date	2020-01-01
Publisher	Sociedade Brasileira de Medicina Tropical - SBMT
Publishing country	br
Document type	Book ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: First clinical study using HCV protease inhibitor danoprevir to treat COVID-19 patients.

Chen, Hongyi / Zhang, Zhicheng / Wang, Li / Huang, Zhihua / Gong, Fanghua / Li, Xiaodong / Chen, Yahong / Wu, Jinzi J

Medicine

2020 Volume 99, Issue 48, Page(s) e23357

Abstract: Introduction: As coronavirus disease 2019 (COVID-19) outbreak globally, repurposing approved drugs is emerging as important therapeutic options. Danoprevir boosted by ritonavir (Ganovo) is a potent hepatitis C virus (HCV) protease (NS3/4A) inhibitor, ... ...

Abstract	Introduction: As coronavirus disease 2019 (COVID-19) outbreak globally, repurposing approved drugs is emerging as important therapeutic options. Danoprevir boosted by ritonavir (Ganovo) is a potent hepatitis C virus (HCV) protease (NS3/4A) inhibitor, which was approved and marketed in China since 2018 to treat chronic hepatitis C patients. Methods: This is an open-label, single arm study evaluating the effects of danoprevir boosted by ritonavir on treatment naïve and experienced COVID-19 patients for the first time. Patients received danoprevir boosted by ritonavir (100 mg/100 mg, twice per day). The primary endpoint was the rate of composite adverse outcomes and efficacy was also evaluated. Results: The data showed that danoprevir boosted by ritonavir is safe and well tolerated in all patients. No patient had composite adverse outcomes during this study. After initiation of danoprevir/ritonavir treatment, the first negative reverse real-time PCR (RT-PCR) test occurred at a median of 2 days, ranging from 1 to 8 days, and the obvious absorption in CT scans occurred at a median 3 days, ranging from 2 to 4 days. After 4 to 12-day treatment of danoprevir boosted by ritonavir, all enrolled 11 patients were discharged from the hospital. Conclusion: Our findings suggest that repurposing danoprevir for COVID-19 is a promising therapeutic option.
MeSH term(s)	Adolescent ; Adult ; Aged ; Antiviral Agents/administration & dosage ; Antiviral Agents/adverse effects ; Antiviral Agents/therapeutic use ; COVID-19/diagnostic imaging ; COVID-19/drug therapy ; Cyclopropanes/administration & dosage ; Cyclopropanes/adverse effects ; Cyclopropanes/therapeutic use ; Drug Therapy, Combination ; Female ; Humans ; Isoindoles/administration & dosage ; Isoindoles/adverse effects ; Isoindoles/therapeutic use ; Lactams, Macrocyclic/administration & dosage ; Lactams, Macrocyclic/adverse effects ; Lactams, Macrocyclic/therapeutic use ; Male ; Middle Aged ; Pandemics ; Proline/administration & dosage ; Proline/adverse effects ; Proline/analogs & derivatives ; Proline/therapeutic use ; Real-Time Polymerase Chain Reaction ; Ritonavir/administration & dosage ; Ritonavir/adverse effects ; Ritonavir/therapeutic use ; SARS-CoV-2 ; Sulfonamides/administration & dosage ; Sulfonamides/adverse effects ; Sulfonamides/therapeutic use ; Tomography, X-Ray Computed ; Young Adult
Chemical Substances	Antiviral Agents ; Cyclopropanes ; Isoindoles ; Lactams, Macrocyclic ; Sulfonamides ; danoprevir (911Z9PCQ5F) ; Proline (9DLQ4CIU6V) ; Ritonavir (O3J8G9O825)
Language	English
Publishing date	2020-11-20
Publishing country	United States
Document type	Clinical Trial ; Journal Article
ZDB-ID	80184-7
ISSN	1536-5964 ; 0025-7974
ISSN (online)	1536-5964
ISSN	0025-7974
DOI	10.1097/MD.0000000000023357
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Article ; Online: Long-term positive severe acute respiratory syndrome coronavirus 2 ribonucleic acid and therapeutic effect of antivirals in patients with coronavirus disease: Case reports.

Wei, Bo / Hang, Xiaofeng / Xie, Ying / Zhang, Yuanjing / Wang, Jianrong / Cao, Xinghao / Wu, Jinzi J / Wang, Junxue

Revista da Sociedade Brasileira de Medicina Tropical

2020 Volume 53, Page(s) e20200372

Abstract: Coronavirus disease (COVID-19), caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has been declared a pandemic. We herein report four COVID-19 cases with long-term positive viral ribonucleic acid (RNA) for about 61 days. Despite ...

Abstract	Coronavirus disease (COVID-19), caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has been declared a pandemic. We herein report four COVID-19 cases with long-term positive viral ribonucleic acid (RNA) for about 61 days. Despite treatment with recombinant human interferon, convalescent plasma from COVID-19 patients, arbidol, etc., nucleic acid results were still positive for SARS-CoV-2. After treatment with ritonavir-boosted danoprevir (DNVr, 100/100 mg, once daily), all four patients showed two to three consecutive negative SARS-CoV-2 RNA and were thus discharged from hospital. Therefore, DNVr may be a potentially effective antiviral for COVID-19 patients with long-term positive SARS-CoV-2 RNA.
MeSH term(s)	Adult ; Aged ; Antiviral Agents/therapeutic use ; Betacoronavirus ; COVID-19 ; Coronavirus ; Coronavirus Infections/drug therapy ; Coronavirus Infections/virology ; Humans ; Male ; Middle Aged ; Pandemics ; Pneumonia, Viral/drug therapy ; Pneumonia, Viral/virology ; RNA, Viral/blood ; SARS-CoV-2 ; COVID-19 Drug Treatment
Chemical Substances	Antiviral Agents ; RNA, Viral
Keywords	covid19
Language	English
Publishing date	2020-07-20
Publishing country	Brazil
Document type	Case Reports ; Journal Article
ZDB-ID	1038126-0
ISSN	1678-9849 ; 0037-8682
ISSN (online)	1678-9849
ISSN	0037-8682
DOI	10.1590/0037-8682-0372-2020
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Zs.A 2726: Show issues

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Article: Comparison of SPA, FRET, and FP for kinase assays.

Wu, Jinzi J

Methods in molecular biology (Clifton, N.J.)

2002 Volume 190, Page(s) 65–85

MeSH term(s)	Amino Acid Sequence ; Animals ; Antibodies ; Drug Design ; Drug Evaluation, Preclinical ; Fluorescence Polarization/methods ; Fluorescence Resonance Energy Transfer/methods ; Humans ; Molecular Biology/methods ; Oligopeptides/chemistry ; Protein Kinase C/analysis ; Protein Kinases/analysis ; Protein Kinases/immunology ; Protein-Serine-Threonine Kinases/analysis ; Protein-Tyrosine Kinases/analysis ; Scintillation Counting ; Substrate Specificity
Chemical Substances	Antibodies ; Oligopeptides ; Protein Kinases (EC 2.7.-) ; Protein-Tyrosine Kinases (EC 2.7.10.1) ; Protein-Serine-Threonine Kinases (EC 2.7.11.1) ; Protein Kinase C (EC 2.7.11.13)
Language	English
Publishing date	2002
Publishing country	United States
Document type	Comparative Study ; Journal Article
ISSN	1064-3745
ISSN	1064-3745
DOI	10.1385/1-59259-180-9:065
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Twelve-week ravidasvir plus ritonavir-boosted danoprevir and ribavirin for non-cirrhotic HCV genotype 1 patients: A phase 2 study.

Kao, Jia-Horng / Yu, Min-Lung / Chen, Chi-Yi / Peng, Cheng-Yuan / Chen, Ming-Yao / Tang, Huoling / Chen, Qiaoqiao / Wu, Jinzi J

Journal of gastroenterology and hepatology

2018 Volume 33, Issue 8, Page(s) 1507–1510

Abstract: Background and aim: The need for all-oral hepatitis C virus (HCV) treatments with higher response rates, improved tolerability, and lower pill burden compared with interferon-inclusive regimen has led to the development of new direct-acting antiviral ... ...

Abstract	Background and aim: The need for all-oral hepatitis C virus (HCV) treatments with higher response rates, improved tolerability, and lower pill burden compared with interferon-inclusive regimen has led to the development of new direct-acting antiviral agents. Ravidasvir (RDV) is a second-generation, pan-genotypic NS5A inhibitor with high barrier to resistance. The aim of this phase 2 study (EVEREST study) was to assess the efficacy and safety of interferon-free, 12-week RDV plus ritonavir-boosted danoprevir (DNVr) and ribavirin (RBV) regimen for treatment-naïve Asian HCV genotype 1 (GT1) patients without cirrhosis. Methods: A total of 38 treatment-naïve, non-cirrhotic adult HCV GT1 patients were enrolled in this multicenter, open-label, single-arm phase 2 study (NCT03020095). All patients received a combination of RDV 200 mg once daily (q.d.) plus DNVr 100 mg/100 mg twice daily (b.i.d.) and oral RBV 1000/1200 mg/day (body weight < 75/≥ 75 kg) for 12 weeks. The primary endpoint was the rate of sustained virologic response 12 weeks after the end of treatment (SVR12). Results: Of 38 patients, all (100%) achieved SVR12. During the study, no treatment-related serious adverse events, no patients discontinued treatment due to adverse events, and no deaths were reported. Six of 37 (16%) patients with available sequences had HCV NS5A resistance-associated variants at baseline. All patients (6/6) with baseline NS5A resistance-associated variants achieved SVR12. Conclusions: Twelve-week RDV and DNVr in combination with RBV for 12 weeks achieves the SVR12 rate of 100% in treatment-naïve non-cirrhotic Asian patients with HCV GT1 infection. This interferon-free regimen is also safe and well tolerated.
MeSH term(s)	Administration, Ophthalmic ; Adult ; Aged ; Aged, 80 and over ; Antiviral Agents ; Asian Continental Ancestry Group ; Drug Administration Schedule ; Drug Therapy, Combination ; Female ; Genotype ; Hepacivirus/genetics ; Hepatitis C, Chronic/drug therapy ; Hepatitis C, Chronic/virology ; Humans ; Lactams/administration & dosage ; Liver Cirrhosis ; Male ; Middle Aged ; Ribavirin/administration & dosage ; Ritonavir/administration & dosage ; Sulfonamides/administration & dosage ; Time Factors ; Treatment Outcome
Chemical Substances	Antiviral Agents ; Lactams ; Sulfonamides ; Ribavirin (49717AWG6K) ; danoprevir (911Z9PCQ5F) ; Ritonavir (O3J8G9O825)
Language	English
Publishing date	2018-03-12
Publishing country	Australia
Document type	Clinical Trial, Phase II ; Journal Article ; Multicenter Study
ZDB-ID	632882-9
ISSN	1440-1746 ; 0815-9319
ISSN (online)	1440-1746
ISSN	0815-9319
DOI	10.1111/jgh.14096
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Zs.A 2180: Show issues			Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular Jg. 1995 - 2021: Lesesall (1.OG) ab Jg. 2022: Lesesaal (EG)
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Article: Long-term positive severe acute respiratory syndrome coronavirus 2 ribonucleic acid and therapeutic effect of antivirals in patients with coronavirus disease: Case reports

Wei, Bo / Hang, Xiaofeng / Xie, Ying / Zhang, Yuanjing / Wang, Jianrong / Cao, Xinghao / Wu, Jinzi J. / Wang, Junxue

Revista da Sociedade Brasileira de Medicina Tropical

Abstract: Coronavirus disease (COVID-19), caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has been declared a pandemic We herein report four COVID-19 cases with long-term positive viral ribonucleic acid (RNA) for about 61 days Despite ... ...

Abstract	Coronavirus disease (COVID-19), caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has been declared a pandemic We herein report four COVID-19 cases with long-term positive viral ribonucleic acid (RNA) for about 61 days Despite treatment with recombinant human interferon, convalescent plasma from COVID-19 patients, arbidol, etc , nucleic acid results were still positive for SARS-CoV-2 After treatment with ritonavir-boosted danoprevir (DNVr, 100/100 mg, once daily), all four patients showed two to three consecutive negative SARS-CoV-2 RNA and were thus discharged from hospital Therefore, DNVr may be a potentially effective antiviral for COVID-19 patients with long-term positive SARS-CoV-2 RNA
Keywords	covid19
Publisher	WHO
Document type	Article
Note	WHO #Covidence: #665936
Database	COVID19

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Article ; Online: First Clinical Study Using HCV Protease Inhibitor Danoprevir to Treat Naive and Experienced COVID-19 Patients

Chen, Hongyi / Zhang, Zhicheng / Wang, Li / Huang, Zhihua / Gong, Fanghua / Li, Xiaodong / Chen, Yahong / WU, Jinzi J.

Abstract: As coronavirus disease 2019 (COVID-19) outbreak, caused by the severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), started in China in January, 2020, repurposing approved drugs is emerging as important therapeutic options. We reported here the ... ...

Abstract	As coronavirus disease 2019 (COVID-19) outbreak, caused by the severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), started in China in January, 2020, repurposing approved drugs is emerging as important therapeutic options. We reported here the first clinical study using hepatitis C virus (HCV) protease inhibitor, danoprevir, to treat COVID-19 patients. Danoprevir (Ganovo) is a potent HCV protease (NS3/4A) inhibitor (IC50 = 0.29 nM), which was approved and marketed in China since 2018 to treat chronic hepatitis C patients. Ritonavir is a CYP3A4 inhibitor to enhance plasma concentration of danoprevir while it also acts as a human immunodeficiency virus (HIV) protease inhibitor at high doses. The chymotrypsin-like protease of SARS-CoV-2 shares structure similarity with HCV and HIV proteases. In the current clinical study (NCT04291729) conducted at the Nineth Hospital of Nanchang, we evaluated therapeutic effects of danoprevir, boosted by ritonavir, on treatment naive and experienced COVID-19 patients. The data from this small-sample clinical study showed that danoprevir boosted by ritonavir is safe and well tolerated in all patients. After 4 to 12-day treatment of danoprevir boosted by ritonavir, all eleven patients enrolled, two naive and nine experienced, were discharged from the hospital as they met all four conditions as follows: (1) normal body temperature for at least 3 days; (2) significantly improved respiratory symptoms; (3) lung imaging shows obvious absorption and recovery of acute exudative lesion; and (4) two consecutive RT-PCR negative tests of SARS-CoV-2 nucleotide acid (respiratory track sampling with interval at least one day). Our findings suggest that repurposing danoprevir for COVID-19 is a promising therapeutic option.
Keywords	covid19
Publisher	MedRxiv; WHO
Document type	Article ; Online
DOI	10.1101/2020.03.22.20034041
Database	COVID19

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Article ; Online: First Clinical Study Using HCV Protease Inhibitor Danoprevir to Treat Naive and Experienced COVID-19 Patients

Chen, Hongyi / Zhang, Zhicheng / Wang, Li / Huang, Zhihua / Gong, Fanghua / Li, Xiaodong / Chen, Yahong / WU, Jinzi J.

medRxiv

Abstract	As coronavirus disease 2019 (COVID-19) outbreak, caused by the severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), started in China in January, 2020, repurposing approved drugs is emerging as important therapeutic options. We reported here the first clinical study using hepatitis C virus (HCV) protease inhibitor, danoprevir, to treat COVID-19 patients. Danoprevir (Ganovo) is a potent HCV protease (NS3/4A) inhibitor (IC50 = 0.29 nM), which was approved and marketed in China since 2018 to treat chronic hepatitis C patients. Ritonavir is a CYP3A4 inhibitor to enhance plasma concentration of danoprevir while it also acts as a human immunodeficiency virus (HIV) protease inhibitor at high doses. The chymotrypsin-like protease of SARS-CoV-2 shares structure similarity with HCV and HIV proteases. In the current clinical study (NCT04291729) conducted at the Nineth Hospital of Nanchang, we evaluated therapeutic effects of danoprevir, boosted by ritonavir, on treatment naive and experienced COVID-19 patients. The data from this small-sample clinical study showed that danoprevir boosted by ritonavir is safe and well tolerated in all patients. After 4 to 12-day treatment of danoprevir boosted by ritonavir, all eleven patients enrolled, two naive and nine experienced, were discharged from the hospital as they met all four conditions as follows: (1) normal body temperature for at least 3 days; (2) significantly improved respiratory symptoms; (3) lung imaging shows obvious absorption and recovery of acute exudative lesion; and (4) two consecutive RT-PCR negative tests of SARS-CoV-2 nucleotide acid (respiratory track sampling with interval at least one day). Our findings suggest that repurposing danoprevir for COVID-19 is a promising therapeutic option.
Keywords	covid19
Language	English
Publishing date	2020-03-24
Publisher	Cold Spring Harbor Laboratory Press
Document type	Article ; Online
DOI	10.1101/2020.03.22.20034041
Database	COVID19

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Article ; Online: Nanoparticles targeted with NGR motif deliver c-myc siRNA and doxorubicin for anticancer therapy.

Chen, Yunching / Wu, Jinzi J / Huang, Leaf

Molecular therapy : the journal of the American Society of Gene Therapy

2010 Volume 18, Issue 4, Page(s) 828–834

Abstract: We have designed a PEGylated LPD (liposome-polycation-DNA) nanoparticle for systemic, specific, and efficient delivery of small interfering RNA (siRNA) into solid tumors in mice by modification with NGR (aspargine-glycine-arginine) peptide, targeting ... ...

Abstract	We have designed a PEGylated LPD (liposome-polycation-DNA) nanoparticle for systemic, specific, and efficient delivery of small interfering RNA (siRNA) into solid tumors in mice by modification with NGR (aspargine-glycine-arginine) peptide, targeting aminopeptidase N (CD13) expressed in the tumor cells or tumor vascular endothelium. LPD-PEG-NGR efficiently delivered siRNA to the cytoplasm and downregulated the target gene in the HT-1080 cells but not CD13(-) HT-29 cells, whereas nanoparticles containing a control peptide, LPD-PEG-ARA, showed only little siRNA uptake and gene silencing activity. LPD-PEG-NGR efficiently delivered siRNA into the cytoplasm of HT-1080 xenograft tumor 4 hours after intravenous injection. Three daily injections (1.2 mg/kg) of c-myc siRNA formulated in the LPD-PEG-NGR effectively suppressed c-myc expression and triggered cellular apoptosis in the tumor, resulting in a partial tumor growth inhibition. When doxorubicin (DOX) and siRNA were co-formulated in LPD-PEG-NGR, an enhanced therapeutic effect was observed.
MeSH term(s)	Animals ; Antibiotics, Antineoplastic/administration & dosage ; Apoptosis ; CD13 Antigens/pharmacology ; Cell Line, Tumor ; Doxorubicin/administration & dosage ; Drug Delivery Systems ; Endothelium, Vascular ; Genes, myc ; HT29 Cells ; Humans ; Liposomes ; Mice ; Mice, Nude ; Nanoparticles/administration & dosage ; Neoplasms/drug therapy ; Oligopeptides/administration & dosage ; RNA, Small Interfering/administration & dosage ; Xenograft Model Antitumor Assays
Chemical Substances	Antibiotics, Antineoplastic ; Liposomes ; NGR peptide ; Oligopeptides ; RNA, Small Interfering ; Doxorubicin (80168379AG) ; CD13 Antigens (EC 3.4.11.2)
Language	English
Publishing date	2010-01-12
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ZDB-ID	2010592-7
ISSN	1525-0024 ; 1525-0016
ISSN (online)	1525-0024
ISSN	1525-0016
DOI	10.1038/mt.2009.291
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