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Last update 04 Apr 2026
Faldaprevir
Last update 04 Apr 2026
Overview
Basic Info
Drug Type Synthetic peptide |
Synonyms Faldaprevir-sodium, 福达瑞韦, BI-201335 + [4] |
Target |
Action inhibitors |
Mechanism NS3/NS4A inhibitors(Hepatitis C virus serine protease, NS3/NS4A inhibitors) |
Therapeutic Areas |
Active Indication- |
Inactive Indication |
Originator Organization |
Active Organization- |
License Organization- |
Drug Highest PhaseDiscontinuedPhase 3 |
First Approval Date- |
Regulation- |
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Structure/Sequence
Molecular FormulaC40H49BrN6O9S |
InChIKeyLLGDPTDZOVKFDU-XUHJSTDZSA-N |
CAS Registry801283-95-4 |
Related
47
Clinical Trials associated with FaldaprevirNCT02716428
A Phase 2, Open-Label Study to Investigate the Safety and Efficacy of Faldaprevir and TD 6450 Alone and in Combination With Other Antivirals for 12 Weeks in Treatment-Naive Patients Chronically Infected With Genotype 1 Hepatitis C Virus
NCT02593162
Phase 2a, Randomized, Double-Blind Study to Investigate the Safety and Efficacy of Faldaprevir in Combination With Ribavirin and TD-6450 for 12 Weeks in Treatment-Naive Patients Chronically Infected With Genotype 4 Hepatitis C Virus
NCT02114671
A Randomised, Assessor-blind, Placebo and Active Controlled, Parallel Group Study to Assess the Phototoxic Potential of Faldaprevir (Administered Orally, Once Daily) for 6 Days in Healthy Male and Female Subjects
100 Clinical Results associated with Faldaprevir
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100 Translational Medicine associated with Faldaprevir
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100 Patents (Medical) associated with Faldaprevir
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141
Literatures (Medical) associated with Faldaprevir01 Jan 2026Clinical Pharmacology in Drug Development
Pharmacokinetics and Pharmacodynamics of Faldaprevir Following Multiple Oral Rising Doses in Healthy Volunteers and Subjects with Gilbert's Syndrome
Article
Author: Elgadi, Mabrouk ; Huang, Fenglei ; Yong, Chan‐Loi ; Quinson, Anne‐Marie ; Wruck, Jan ; Cooper, Curtis L
Abstract:
Faldaprevir (FDV) is an investigational NS3/NS4A protease inhibitor for chronic hepatitis C. This study evaluated the safety, tolerability, and pharmacokinetics (PK) of FDV after multiple rising doses in healthy male volunteers and subjects with Gilbert syndrome (GS). In this randomized, double‐blind, placebo‐controlled study, healthy males received once‐daily oral FDV (20, 48, 120 mg [
n
= 6 per group], 240 mg [
n
= 5]), or placebo (
n
= 7). A single dose was given on Day 1, followed by a 72‐h washout and 21 days of dosing from day 4. Separately, 9 GS subjects received open‐label FDV 240 mg daily for 28 days. PK was assessed after the first and last doses; safety was evaluated throughout. FDV showed greater than dose‐proportional increases in exposure (gMean
Cmax,ss
: 99–5360 ng/mL; AUC
τ,ss
: 1740–50,100 h·ng/mL) and time‐dependent PK with a linearity index >1. Mean
t1/2
was 20–30 h; steady state was reached in 6–7 days with an accumulation ratio of 2.8–3.1. FDV exposure in GS subjects was similar but slightly lower. Total bilirubin increased dose‐dependently, with higher indirect bilirubin in GS subjects. FDV exhibited non‐linear, time‐dependent PK and was generally well tolerated up to 240 mg/day in subjects with or without GS.
02 Jun 2025MOLECULAR PHARMACEUTICS
Beyond Barriers, Big Crystallization Hurdles: Atropisomerism in Beyond Rule of Five Compounds Explored by Computational and NMR Studies
Article
Author: Werthmann, Ulrike ; Schneider, Regina ; Ries, Benjamin ; Montel, Florian ; Jandl, Christian ; Stamos, Nikolaos Angelos ; Tzvetkova, Pavleta
Stereochemical purity, stability, and selection of a suitable solid-state form are pivotal factors in pharmaceutical development, particularly for complex beyond Rule of 5 (bRo5) compounds. In this study, we explore the intricate interplay between atropisomerism and crystallization using two model bRo5 compounds, namely, ACBI1 and BI201335, both violating three of four Lipinski's rules. One of the tool compounds exhibits Class 2 atropisomeric behavior, and the other is devoid of it. A diverse array of crystallization methods, including solution-phase crystallization, cocrystallization, and salt formation, were applied, revealing the critical role of atropisomerism-induced stereochemistry in polymorphism and nucleation outcomes. In silico torsion profile calculations and NMR studies were employed to elucidate the rotational energy barriers and confirm the presence or absence of atropisomerism. This comprehensive analysis highlights the significance of understanding stereochemical phenomena such as atropisomerism in designing and developing bRo5 compounds. By integrating advanced analytical techniques and crystallization strategies, this work provides novel insights into tailoring pharmaceutical properties for next-generation therapeutics.
01 Jun 2025FLUID PHASE EQUILIBRIA
Acidic deep eutectic systems and their capacity to increase drug bioavailability
Author: Fernandes, Claudio C. ; Ferreira, Ines J. ; Duarte, Ana Rita C.
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.
100 Deals associated with Faldaprevir
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External Link
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | Faldaprevir |
R&D Status
10 top R&D records. to view more data
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| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| Chronic hepatitis C genotype 1b | Phase 3 | Australia | 01 May 2013 | |
| Chronic hepatitis C genotype 1b | Phase 3 | Spain | 01 May 2013 | |
| Chronic hepatitis C genotype 1b | Phase 3 | Sweden | 01 May 2013 | |
| Chronic hepatitis C genotype 1 | Phase 3 | United States | 01 Apr 2011 | |
| Chronic hepatitis C genotype 1 | Phase 3 | Japan | 01 Apr 2011 | |
| Chronic hepatitis C genotype 1 | Phase 3 | Austria | 01 Apr 2011 | |
| Chronic hepatitis C genotype 1 | Phase 3 | Belgium | 01 Apr 2011 | |
| Chronic hepatitis C genotype 1 | Phase 3 | Canada | 01 Apr 2011 | |
| Chronic hepatitis C genotype 1 | Phase 3 | France | 01 Apr 2011 | |
| Chronic hepatitis C genotype 1 | Phase 3 | Germany | 01 Apr 2011 |
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Clinical Result
Clinical Result
Indication
Phase
Evaluation
View All Results
Phase 3 | 131 | faldaprevir 120 mg | zrkgpaejkn(ygaodlptad) = mxdyecojcm ijvitarove (ybezghntcg ) | - | 01 Mar 2017 | ||
faldaprevir 240 mg 12 weeks | zrkgpaejkn(ygaodlptad) = dnymexdtsr ijvitarove (ybezghntcg ) | ||||||
Phase 2 | 35 | (moderate hepatic impairment（Child-Pugh B [CPB]）) | riwwatkiqi(pdqksetstz) = sevounwljq eoxfrtlywy (frpbhodgxl, 29.2 - 76.7) View more | Positive | 28 Dec 2016 | ||
(mild hepatic impairment（Child-Pugh A [CPA]）) | riwwatkiqi(pdqksetstz) = obdiacxpse eoxfrtlywy (frpbhodgxl, 38.6 - 83.6) View more | ||||||
Phase 1 | 72 | lqfcgfavjh(pupjyyvyyy) = icuvvtbmst cmvfeextnl (eundjxznhp, 54.8) View more | - | 10 Jun 2016 | |||
lqfcgfavjh(pupjyyvyyy) = yrtpebpsvh cmvfeextnl (eundjxznhp, NA) View more | |||||||
Phase 3 | 470 | FDV+RBV (24 wk FDV+DBV+RBV) | iszcyomlfi = renfzrruil xtcaeqllfz (ezmqguktlk, wywoafaaju - keyxacwfvk) View more | - | 18 Apr 2016 | ||
DBV+RBV (16 wk FDV+DBV+RBV) | iszcyomlfi = gwefkbvdkr xtcaeqllfz (ezmqguktlk, ruurcrvuct - tawckyogup) View more | ||||||
Phase 1 | - | 48 | (BI 207127+ Faldaprevir) | dlijwaobns(ffayvoyhec) = xfuubuyhop fdjtlvmhlg (eykpmgazxe, 1.65) View more | - | 14 Apr 2016 | |
(Placebo to BI 207127 + Placebo to Faldaprevir) | dlijwaobns(ffayvoyhec) = ijcqfgnozx fdjtlvmhlg (eykpmgazxe, 1.64) View more | ||||||
Phase 2 | 25 | (600mg Deleobuvir and 80mg Faldaprevir) | buuvtmignb = lplncbempw ayzegdsgtw (wycccxccjj, gcslviduur - fapbvohkme) View more | - | 13 Apr 2016 | ||
(600mg Deleobuvir and 120mg Faldaprevir) | buuvtmignb = uvggqljtgl ayzegdsgtw (wycccxccjj, xodpmyesxg - ikwydqogvr) View more | ||||||
Phase 1 | - | 18 | bwdtnaystw(ztnadfzlej) = qnqpuuhkvz zpzabvcuyj (hcpjaglpwo, sisefvmyqh - dlesgmypir) View more | - | 11 Apr 2016 | ||
Phase 1 | 4 | eaygnwmljq = sffuztzlwl klzutsoluo (uuncjzsscr, sxorkzagsd - jogndlivsk) View more | - | 11 Apr 2016 | |||
Phase 1 | - | 32 | (400 mg Deleobuvir) | aevjnxmjmu = ouprfcfxsy vfpmgtlsbo (jefvhcwgvs, huszonnhuc - sbijaethlh) View more | - | 08 Apr 2016 | |
(600 mg Deleobuvir) | aevjnxmjmu = sfieqdiadm vfpmgtlsbo (jefvhcwgvs, zfomseesdh - rzsqfxlgcc) View more | ||||||
Phase 3 | 118 | (prior relapsers) | amvigfjrzl(qzmmjvojvw) = rqnfovqvfh hadkggsfor (hfmhdepkid, 89.1 - 100.0) View more | Positive | 01 Mar 2016 | ||
(prior nonresponders (null responders, partial responders and patients with breakthrough)) | amvigfjrzl(qzmmjvojvw) = vegzoiiuda hadkggsfor (hfmhdepkid, 43.4 - 65.9) View more |
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