Delving into the Latest Updates on Faldaprevir with Synapse

Overview

Basic Info

Drug Type

Synthetic peptide

Synonyms

Faldaprevir-sodium, 福达瑞韦

+ [4]

Target

NS3/NS4A

Action

inhibitors

Mechanism

NS3/NS4A inhibitors(Hepatitis C virus serine protease, NS3/NS4A inhibitors)

Therapeutic Areas

Infectious DiseasesDigestive System DisordersImmune System Diseases+ [5]

Active Indication-

Inactive Indication

Chronic hepatitis C genotype 1Chronic hepatitis C genotype 1bCompensated cirrhosis+ [5]

Originator Organization

Boehringer Ingelheim GmbH

Active Organization-

Inactive Organization

Boehringer Ingelheim GmbH

Trek Therapeutics PBC

Boehringer Ingelheim International GmbH

License Organization-

Drug Highest PhaseDiscontinuedPhase 3

First Approval Date-

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC40H49BrN6O9S

InChIKeyLLGDPTDZOVKFDU-XUHJSTDZSA-N

CAS Registry801283-95-4

To investigate the potential of Faldaprevir to induce skin phototoxicity, immediate or delayed type, to UV light and visible light in healthy male and female subjects. To investigate the degree, wavelength dependency, severity, pigmentation and morphology of the phototoxic effects. The persistence of the phototoxic susceptibility will be explored following cessation of study medication. Within a sunscreen sub-study, the efficacy of commercially available high factor sunscreen will also be assessed in terms of its potential to prevent any phototoxic skin responses seen. The safety and tolerability of Faldaprevir will also be assessed.

Start Date01 Apr 2014

Sponsor / Collaborator

Boehringer Ingelheim GmbH

100 Clinical Results associated with Faldaprevir

Login to view more data

100 Translational Medicine associated with Faldaprevir

Login to view more data

100 Patents (Medical) associated with Faldaprevir

Login to view more data

162

Literatures (Medical) associated with Faldaprevir

01 Jun 2025·Fluid Phase Equilibria

Acidic deep eutectic systems and their capacity to increase drug bioavailability

Author: Duarte, Ana Rita C. ; Fernandes, Claudio C. ; Ferreira, Ines J.

The pharmaceutical industry faces several challenges concerning the bioavailability of novel medications mainly because of their limited permeability and/or solubilityThese are two crucial features that influence how well a medication is absorbed.The biopharmaceutics categorization system is a crucial instrument for the classification of active pharmaceutical ingredients (API) based on their permeability and solubilityIn this work we explored the possibility of deep eutectic systems (DES) to be used as solubility and permeability enhancers of four different drugs supplied by Boeringher Ingelheim.In this investigation, the API′s were dissolved in various DES and their solubility measured in PBS at 37 °C.Our findings suggest that CA: Gly: W (1:1:1) was able to increase the solubility of all four drugs in PBS, as well as their permeability.In summary, BI0001 and BI0002 following pre-solubilization in that system drugs shifted from class III to from class I included, whereas BI0005 still kept its class III classification although having higher solubility and permeability.The encouraging outcomes highlight DES′s potential as a technique to boost drug′s bioavailability.

18 Sep 2024·ChemistrySelect

Computational Screening of FDA‐Approved Hepatitis C Drugs for Inhibition of VEGFR2 in Liver Cancer

Author: Aluwi, Mohd Fadhlizil Fasihi Mohd ; Tufail, Nasir ; Wilhelm, Anke ; Issahaku, Abdul Rashid ; Roney, Miah

AbstractLiver cancer (LC) is one of the most common tumours and the leading cause of cancer‐related death globally. Amidst the problems associated with existing treatments, such as hepatotoxicity, recurrence, drug resistance, and other adverse effects, researchers are under pressure to find alternatives. Towards a comprehensive rationalisation of the search for new anti‐LC drugs among approved ones, we employed an in‐silico approach to accelerate the selection of the most efficacious LC drugs. The FDA‐approved hepatitis C virus (HCV) drugs were docked with the LC protein using the AutoDock Vina software. Compared to the control compound, two FDA‐approved HCV drugs (DB09102 and DB09027) were selected based on their binding energies and interactions with the target protein, which showed comparable binding energies. Furthermore, these compounds were then subjected to molecular dynamic simulation, principle component analysis, and MMGBSA using the AMBER20 software, and the results showed stable complexes compared to the control complex. All things considered, this study will help the scientific community and society find a novel drug to treat LC.

30 Sep 2023·Diagnostics (Basel, Switzerland)

Molecular Mechanisms of Resistance to Direct-Acting Antiviral (DAA) Drugs for the Treatment of Hepatitis C Virus Infections.

Article

Author: Izhari, Mohammad Asrar

Hepatitis C virus (HCV) is a hepatotropic virus that affects millions of human lives worldwide. Direct-acting antiviral (DAA) regimens are the most effective HCV treatment option. However, amino acid substitution-dependent resistance to DAAs has been a major challenge. This study aimed to determine the increasing risk of DAA resistance due to substitutions in DAA target non-structural proteins (NS3/4A, NS5A, and NS5B). Using a Sequence Retrieval System (SRS) at the virus pathogen resource (ViPR/BV-BRC), n = 32763 target protein sequences were retrieved and analyzed for resistance-associated amino acid substitutions (RAASs) by the Sequence Feature Variant Type (SFVT) antiviral-resistance assessment modeling tool. Reference target protein sequences with 100% identity were retried from UniProt following NCBI BLAST. The types and locations of RAASs were identified and visualized by AlphaFold and PyMol. Linux-r-base/R-studio was used for the data presentation. Multi-drug-resistant variants of NS3/4A in genotype 1 (n = 9) and genotype 5 (n = 5) along with DAA-specific NS3/4A, NS5A, and NS5B variants were identified pan-genotypically. A total of 27 variants (RAASs) of all the targets were identified. Fourteen genotype 1-specific substitutions: V1196A, V1158I, D1194A/T/G, R1181K, T1080S, Q1106R, V1062A, S1148G, A1182V, Y2065N, M2000T, and L2003V were identified. The most frequent substitutions were V1062L and L2003M, followed by Q2002H. L2003V, Q2002H, M2000T, Y2065N, and NL2003M of NS5A and L2003M of NS5B conferred resistance to daclatasvir. S2702T NS5B was the sofosbuvir-resistant variant. D1194A NS3/4A was triple DAA (simeprevir, faldaprevir, and asunaprevir) resistant. The double-drug resistant variants R1181K (faldaprevir and asunaprevir), A1182V and Q1106K/R (faldaprevir and simeprevir), T1080S (faldaprevir and telaprevir), and single drug-resistant variants V1062L (telaprevir), D1194E/T (simeprevir), D1194G (asunaprevir), S1148A/G (simeprevir), and Q1106L (Boceprevir) of NS3/4A were determined. The molecular phenomenon of DAA resistance is paramount in the development of HCV drug candidates. RAASs in NS3, NS5A, and NS5B reduce the susceptibility to DAAs; therefore, continuous RAAS-dependent resistance profiling in HCV is recommended to minimize the probability of DAA therapeutic failure.

100 Deals associated with Faldaprevir

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
-	Faldaprevir	J05AP04	DB11808

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Chronic hepatitis C genotype 1	Phase 3	Russia	Boehringer Ingelheim GmbH	01 Apr 2011
Chronic hepatitis C genotype 1	Phase 3	Japan	Boehringer Ingelheim GmbH	01 Apr 2011
Chronic hepatitis C genotype 1	Phase 3	Japan	Boehringer Ingelheim GmbH	01 Apr 2011
Chronic hepatitis C genotype 1	Phase 3	Germany	Boehringer Ingelheim GmbH	01 Apr 2011
Chronic hepatitis C genotype 1	Phase 3	South Korea	Boehringer Ingelheim GmbH	01 Apr 2011
Chronic hepatitis C genotype 1	Phase 3	Austria	Boehringer Ingelheim GmbH	01 Apr 2011
Chronic hepatitis C genotype 1	Phase 3	Austria	Boehringer Ingelheim GmbH	01 Apr 2011
Chronic hepatitis C genotype 1	Phase 3	Russia	Boehringer Ingelheim GmbH	01 Apr 2011
Chronic hepatitis C genotype 1	Phase 3	South Korea	Boehringer Ingelheim GmbH	01 Apr 2011
Chronic hepatitis C genotype 1	Phase 3	Germany	Boehringer Ingelheim GmbH	01 Apr 2011

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01830127 (HCVerso3, Pubmed \| J Biol Chem \| PLoS One) Manual	Phase 2	Fibrosis \| Hepatitis C	35	Faldaprevir+Deleobuvir+Ribavirin (moderate hepatic impairment（Child-Pugh B [CPB]）)	(jegeexqypi) = lotvfvsxoi keiukrogkd (prrpjiwssn, 29.2 - 76.7) View more	Positive	28 Dec 2016
				Faldaprevir+Deleobuvir+Ribavirin (mild hepatic impairment（Child-Pugh A [CPA]）)	(jegeexqypi) = szmfddulis keiukrogkd (prrpjiwssn, 38.6 - 83.6) View more
NCT01525628 (CTgov)	Phase 1	Chronic hepatitis C genotype 1	72	pegylated interferon+BI 207127+BI 201335+tolbutamide+midazolam+caffeine+ribavirin (Group A)	bfilwncvsn(zpwbvejrdu) = thwebhkdsq hkpypsgskb (kxkelgdqpd, tzlkbxjsqe - ebchinadnc) View more	-	10 Jun 2016
				pegylated interferon+BI 207127+BI 201335+tolbutamide+midazolam+caffeine+ribavirin (Group B)	bfilwncvsn(zpwbvejrdu) = zuuzlixnkt hkpypsgskb (kxkelgdqpd, jyufywdpxn - tdpqaudobe) View more
NCT01965431 (CTgov)	Phase 1	-	48	BI 207127+Faldaprevir (BI 207127+ Faldaprevir)	hfcuagozby(bppbnbnzda) = jaetxbwpxj lsgynemmys (mwpczgwpiu, hgnmxqnzyd - fijrkynope) View more	-	14 Apr 2016
				Placebo+BI 207127+Faldaprevir (Placebo to BI 207127 + Placebo to Faldaprevir)	hfcuagozby(bppbnbnzda) = uvndotwmhq lsgynemmys (mwpczgwpiu, czecrrclri - bfkpkxvjzh) View more
NCT01528735 (CTgov)	Phase 2	Hepatitis C, Chronic	25	Deleobuvir+Faldaprevir (600mg Deleobuvir and 80mg Faldaprevir)	eoktqyweoj(qdsstfwilb) = aahqbmgpsa svmfgcbbfs (myhsewydsw, qriiyfyxxu - atxoqfeunh) View more	-	13 Apr 2016
				Deleobuvir+Faldaprevir (600mg Deleobuvir and 120mg Faldaprevir)	eoktqyweoj(qdsstfwilb) = eyxxtvyvfs svmfgcbbfs (myhsewydsw, fjjzyucovy - ronptdvfti) View more
NCT01941615 (CTgov)	Phase 1	-	18	Deleobuvir+Faldaprevir+Microgynon	qqzlwakjfj(rcbphchjeg) = joqmimspmm qjeemnvcfg (sxrzgbomrg, hwgokbuvcz - ntvocepfcx) View more	-	11 Apr 2016
NCT01957657 (CTgov)	Phase 1	Renal Insufficiency	4	Deleobuvir+Faldaprevir	ksvilxyscb(tdxxzlupby) = mxechcxlix aqqepfxgwc (rmrlxjmjfe, gamtkwskvh - rcxlqarfnq) View more	-	11 Apr 2016
NCT01737996 (CTgov)	Phase 1	-	32	Deleobuvir (400 mg Deleobuvir)	oypogulwtk(yadvthzamr) = kqxpnquwwx yavjvbcuhc (klnepimgis, sxfbtgkawa - hiazsvgbop) View more	-	08 Apr 2016
				Deleobuvir (600 mg Deleobuvir)	oypogulwtk(yadvthzamr) = xwemvkxrmz yavjvbcuhc (klnepimgis, fxduxcudhb - okprlmnvvo) View more
NCT01330316 (Pubmed \| J Viral Hepat) Manual	Phase 3	Hepatitis C	118	peginterferon+ribavirin+faldaprevir (prior relapsers)	(mbhnbaqbhy) = fckvpbghrz nbczqxcbhs (vxodlsgbro, 89.1 - 100.0) View more	Positive	01 Mar 2016
				peginterferon+ribavirin+faldaprevir (prior nonresponders (null responders, partial responders and patients with breakthrough))	(mbhnbaqbhy) = thgansndka nbczqxcbhs (vxodlsgbro, 43.4 - 65.9) View more
NCT01528735 (Pubmed \| Hepatol Res) Manual	Phase 2	Chronic hepatitis C genotype 1 First line	25	deleobuvir+ribavirin+peginterferon-α-2a+faldaprevir 80mg	(crmygardej) = ertfanlmje dzhgfreoil (hcqmtmqqnf ) View more	Positive	01 Mar 2016
				deleobuvir+ribavirin+peginterferon-α-2a+faldaprevir 120mg	(crmygardej) = jnjiaufnvw dzhgfreoil (hcqmtmqqnf ) View more
NCT00774397 (CTgov)	Phase 2	Hepatitis C, Chronic	719	BI 201335 NA 120mg QD / LI+PegIFN/RBV (120 mg QD / LI-TN)	xokiwrwdce(xwvnngqlvo) = adurlpeyaf rpatykzzcu (vhuxrcacre, bvlbnrzapy - knsxwtvpco) View more	-	16 Nov 2015
				BI 201335 NA 240 mg QD / LI+PegIFN/RBV (240 mg QD / LI-TN)	xokiwrwdce(xwvnngqlvo) = dqewcmxrwy rpatykzzcu (vhuxrcacre, jhknbjlrik - rayakovffo) View more

Login to view more data

Translational Medicine

Boost your research with our translational medicine data.

login

or

view full example data

Boost your research with our translational medicine data.

Deal

Boost your decision using our deal data.

login

or

view full example data

Boost your decision using our deal data.

Core Patent

Boost your research with our Core Patent data.

login

or

view full example data

Boost your research with our Core Patent data.

Clinical Trial

Identify the latest clinical trials across global registries.

login

or

view full example data

Identify the latest clinical trials across global registries.

Approval

Accelerate your research with the latest regulatory approval information.

login

or

view full example data

Accelerate your research with the latest regulatory approval information.

Biosimilar

Competitive landscape of biosimilars in different countries/locations. Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3.

login

or

view full example data

Competitive landscape of biosimilars in different countries/locations. Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3.

Regulation

Understand key drug designations in just a few clicks with Synapse.

login

or

view full example data

Understand key drug designations in just a few clicks with Synapse.

Faldaprevir

Overview

Basic Info

Structure/Sequence

Related

External Link

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Biosimilar

Regulation