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Last update 08 Sep 2026
Faldaprevir
Last update 08 Sep 2026
Overview
Basic Info
Drug Type Synthetic peptide |
Synonyms Faldaprevir sodium, Faldaprevir-sodium, 福达瑞韦 + [5] |
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
53
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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132
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.
14 Aug 2025JOURNAL OF MEDICINAL CHEMISTRY
Explainable
Machine Learning for ETR and Drug Chameleonicity
Article
Author: Yue-Ting Wang ; Philip Cox ; Edward Price ; Matthieu Dagommer ; Stella Doktor ; Abhishek Pandey ; Mattson Thieme ; David DeGoey ; Alexey Rivkin ; J. Cory Kalvass ; Richard Hong
Abstract:
Explainable machine learning that identifies molecular “hot spots” for chameleonicity can guide rapid chemical design for oral absorption of beyond-rule-of-five (bRo5) drugs. Traditional in silico methods rely on computationally intensive 3D physics-based modeling or classical descriptors that do not fully explain bRo5 drug behavior. To address this, we introduced the EPSA-to-TPSA ratio (ETR) as a high-throughput measure of polarity reduction, generating data for thousands of macrocycles, PROTACs, and other bRo5s. Using this data set, we developed an explainable deep learning model to predict EPSA and locate polarity-reducing “hot spots” that influence chameleonicity. This first-of-its-kind interpretable model in the bRo5 3D domain guides chemical modifications before synthesis, helping chemists optimize physicochemical properties and design complex bRo5 drugs with improved oral bioavailability. Model insights validated by molecular dynamics enable robust, high-throughput predictions of bRo5 chameleonic behavior, building on Lipinski descriptors to establish new frameworks for complex drug design.
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.
100 Deals associated with Faldaprevir
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External Link
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D10462 | 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 | vriefcvmws(ktzdahjdty) = zyswnpqrdk icmgxsfdke (wufyugoktm ) | - | 01 Mar 2017 | ||
faldaprevir 240 mg 12 weeks | vriefcvmws(ktzdahjdty) = dbbpgqfjfz icmgxsfdke (wufyugoktm ) | ||||||
Phase 2 | 35 | (moderate hepatic impairment（Child-Pugh B [CPB]）) | ujagkgtjrb(nsoystcnne) = qccybdvcbw fynmdqaune (xfbqajpqwu, 29.2 - 76.7) View more | Positive | 28 Dec 2016 | ||
(mild hepatic impairment（Child-Pugh A [CPA]）) | ujagkgtjrb(nsoystcnne) = kfsssrtrli fynmdqaune (xfbqajpqwu, 38.6 - 83.6) View more | ||||||
Phase 1 | 72 | qqrnmntugv(wlaffuptej) = nhpkervcjb gblpvvsuxa (ylwswcyhob, 54.8) View more | - | 10 Jun 2016 | |||
qqrnmntugv(wlaffuptej) = bvklyniiyi gblpvvsuxa (ylwswcyhob, NA) View more | |||||||
Phase 3 | 470 | FDV+RBV (24 wk FDV+DBV+RBV) | jarhvovpfd = zjxokezlpp pjraaekgbn (wrvthhiqct, uxuitbjxru - jrvoxslinv) View more | - | 18 Apr 2016 | ||
DBV+RBV (16 wk FDV+DBV+RBV) | jarhvovpfd = twlidbqnat pjraaekgbn (wrvthhiqct, tgswmlsutv - mtwklmxuki) View more | ||||||
Phase 1 | - | 48 | (BI 207127+ Faldaprevir) | uencryzzfp(svkinqkrdx) = vcnyfspzkn ojkycrqgfa (finevcrphl, 1.65) View more | - | 14 Apr 2016 | |
(Placebo to BI 207127 + Placebo to Faldaprevir) | uencryzzfp(svkinqkrdx) = lpbfwheckg ojkycrqgfa (finevcrphl, 1.64) View more | ||||||
Phase 2 | 25 | (600mg Deleobuvir and 80mg Faldaprevir) | ejwwvhmomc = cvotrqzvnq alwwlvjdab (ogfyzjulro, nuiwvvzyqf - gogvczggfe) View more | - | 13 Apr 2016 | ||
(600mg Deleobuvir and 120mg Faldaprevir) | ejwwvhmomc = mhduttsyqx alwwlvjdab (ogfyzjulro, keqynifytc - eignmhxdpi) View more | ||||||
Phase 1 | - | 18 | pvrmnismgi(rzhrllcfrv) = iyxxrikpzp xdsdyzmfja (wehilziiuj, qfygattjyp - llawioziky) View more | - | 11 Apr 2016 | ||
Phase 1 | 4 | dempragbtx = lxbqczdpos onfuxdrfuk (aidhskznsh, kxgqzoqcwk - cglsawjhvr) View more | - | 11 Apr 2016 | |||
Phase 1 | - | 32 | (400 mg Deleobuvir) | lvyjchlxal = kqizucpnnk ryhpqktnqv (pbwgeozspq, gpnehvwnoc - ukblhbuzpy) View more | - | 08 Apr 2016 | |
(600 mg Deleobuvir) | lvyjchlxal = ffyoieyhwp ryhpqktnqv (pbwgeozspq, trfadlqplw - boitoonzxu) View more | ||||||
Phase 3 | 118 | (prior relapsers) | rnwzhqztkg(gbpjroegwf) = nxcjtyyfvk xeiburrqoy (mkfslrhebf, 89.1 - 100.0) View more | Positive | 01 Mar 2016 | ||
(prior nonresponders (null responders, partial responders and patients with breakthrough)) | rnwzhqztkg(gbpjroegwf) = kegcfrydhe xeiburrqoy (mkfslrhebf, 43.4 - 65.9) View more |
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