Faldaprevir

Summary

Faldaprevir (CHEMBL1241348) is a phase-3 clinical-stage small molecule (ATC J05AP04); indicated across 5 conditions including chronic hepatitis c virus infection and hepatitis c virus infection.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: J05AP04
• Indications: 5 conditions
• Clinical trials: 29
• Chemistry: 869.8 Da · C40H49BrN6O9S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1241348
Name	Faldaprevir
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	42601552
ATC	J05AP04
Molecular formula	C40H49BrN6O9S
Molecular weight	869.8
InChIKey	LLGDPTDZOVKFDU-XUHJSTDZSA-N

SMILES: CC(C)C(=O)NC1=NC(=CS1)C2=NC3=C(C=CC(=C3Br)OC)C(=C2)O[C@@H]4C[C@H](N(C4)C(=O)[C@H](C(C)(C)C)NC(=O)OC5CCCC5)C(=O)N[C@@]6(C[C@H]6C=C)C(=O)O

IUPAC name: trans-(1R,2S)-1-[[(2S,4R)-4-[8-bromo-7-methoxy-2-[2-(2-methylpropanoylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy-1-[(2S)-2-(cyclopentyloxycarbonylamino)-3,3-dimethylbutanoyl]pyrrolidine-2-carbonyl]amino]-2-ethenylcyclopropane-1-carboxylic acid

Also known as: BI 201335, BI-201335, BI201335, Faldaprevir, Faldaprevirr, FALDAPREVIR

Parent form; salt/anhydrous children: CHEMBL3544915

Patent coverage: 151 distinct patent families (397 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 396 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Cathepsin E, Sterol O-acyltransferase 2, Cathepsin B, Serine/threonine protein phosphatase PP2B-alpha catalytic subunit.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 4 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
Q7TQM4	5.62	IC50	2400	nM	CHEMBL_ACT_5217592
PPP3CB	5.05	IC50	9000	nM	CHEMBL_ACT_5217593

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

5 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
chronic hepatitis C virus infection	3	MONDO:0005354	EFO:0004220
hepatitis C virus infection	3	MONDO:0005231	EFO:0003047
viral infectious disease	3	MONDO:0005108	EFO:0000763
HIV infectious disease	1	MONDO:0005109	EFO:0000764
kidney failure	1	MONDO:0001106	HP:0000083

Clinical trials

Total trials: 29.

Phase distribution

Phase	Trials
PHASE1	16
PHASE3	7
PHASE2	6

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01297270	PHASE3	COMPLETED	Efficacy and Safety of BI 201335 (Faldaprevir) in Combination With Pegylated Interferon-alpha and Ribavirin in Treatment-naïve Genotype 1 Hepatitis C Infected Patients (STARTverso 2)
NCT01330316	PHASE3	COMPLETED	A Rollover Study of BI 201335 in Combination With Pegylated Interferon-alpha and Ribavirin in Treatment-experienced Genotype 1 Hepatitis C Infected Patients
NCT01343888	PHASE3	COMPLETED	Efficacy and Safety of BI 201335 (Faldaprevir) in Combination With Pegylated Interferon-alpha and Ribavirin in Treatment-naïve Genotype 1 Hepatitis C Infected Patients (STARTverso 1)
NCT01358864	PHASE3	COMPLETED	Efficacy and Safety of BI 201335 (Faldaprevir) in Combination With Pegylated Interferon-alpha and Ribavirin in Treatment-Experienced Genotype 1 Hepatitis C Infected Patients (STARTverso 3)
NCT01399619	PHASE3	COMPLETED	Phase III Trial of BI 201335 (Faldaprevir) in Treatment Naive (TN) and Relapser Hepatitis C Virus (HCV)-Human Immunodeficiency Virus (HIV) Coinfected Patients (STARTverso 4)
NCT01608737	PHASE3	WITHDRAWN	A Phase III Study of BI201335 in Treatment-naive and Prior Relapser Patients With Chronic Hepatitis C Infection
NCT01858961	PHASE3	WITHDRAWN	Open Label Trial to Compare BI 207127 to Telaprevir in HCV Patients
NCT00984620	PHASE2	COMPLETED	Short Term Treatment With BI 201335, Peginterferon-alpha 2a and Ribavirin in Hepatitis c Virus Genotype-1 Treatment-naïve Patients (SILEN-C3)
NCT01132313	PHASE2	COMPLETED	Safety, Antiviral Effect and PK of BI 207127 + BI 201335 +/- RBV for 4 up to 40 Weeks in Patients With Chronic HCV Genotype 1 Infection
NCT01830127	PHASE2	COMPLETED	BI 207127 / Faldaprevir Combination Therapy in Hepatic Impairment (Child-Pugh B) Patients With Genotype 1b Chronic Hepatitis C Infection: HCVerso3
NCT01859962	PHASE2	COMPLETED	Study of PPI-668, BI 207127 and Faldaprevir, With and Without Ribavirin, in the Treatment of Chronic Hepatitis C
NCT02593162	PHASE2	COMPLETED	A Study of Faldaprevir, Ribavirin and TD-6450 in Participants With Genotype 4 Hepatitis C Virus Infection
NCT02716428	PHASE2	COMPLETED	A Study of Faldaprevir, TD-6450 and Other Antivirals in Participants With Genotype 1b Hepatitis C Virus Infection
NCT00793793	PHASE1	COMPLETED	Safety, Antiviral Activity and PK of MRD of BI 201335 in Chronic Hepatitis C Patients Both Treatment Naive and -Experienced
NCT01340196	PHASE1	COMPLETED	Drug Drug Interaction of BI 201335 and Tenofovir
NCT01374802	PHASE1	COMPLETED	Effect of Multiple Dosing With BI 201335 on the Pharmacokinetics of Darunavir Co-administered With Ritonavir in Healthy Male and Female Volunteers
NCT01525628	PHASE1	COMPLETED	Drug Drug Interaction Study Between BI 201335 and BI 207127 in Chronic Hepatitis C Infected Patients
NCT01570244	PHASE1	COMPLETED	Drug-drug Interaction of BI 201335 and Microgynon
NCT01580306	PHASE1	COMPLETED	Pharmacokinetics and Safety of BI 201335 in Patients With Mild to Severe Renal Impairment
NCT01637922	PHASE1	COMPLETED	Drug Interaction Study With BI 201335 and Methadone or Buprenorphine/Naloxone
NCT01694706	PHASE1	COMPLETED	Investigation of Food Effect and Gastric ph Increase on the Bioavailability of Faldapravir
NCT01737996	PHASE1	COMPLETED	Safety, Tolerability and Pharmacokinetics of Different Multiple Doses of BI 207127 BID and Multiple Doses of BI 207127 Combined With Faldaprevir in Healthy Male and Female Subjects
NCT01785160	PHASE1	COMPLETED	Investigation of Faldaprevir Effect on Pharmacokinetics of Raltegravir
NCT01795937	PHASE1	COMPLETED	Investigation of Interactions Between Faldaprevir, Itraconazole, Atorvastatin and Rosuvastatin
NCT01909778	PHASE1	COMPLETED	Open Label Single Dose Phase I Trial of BI 201335 to Study Pharmacokinetics and Safety in Patients With Compensated Liver Cirrhosis
NCT01941615	PHASE1	TERMINATED	Effect of BI 207127 + Faldaprevir on Blood Levels of Oral Contraceptives Containing Ethinylestradiol and Levonorgestrel
NCT01957657	PHASE1	TERMINATED	Pharmacokinetics, Safety and Tolerability of the Combination of BI 207127 and Faldaprevir in Renal Impaired Patients
NCT01965431	PHASE1	COMPLETED	Thorough QT Study to Evaluate the Effects of BI 207127 (Deleobuvir) Combined With Faldaprevir on Cardiac Safety Parameters in Healthy Subjects.
NCT02016625	PHASE1	COMPLETED	Investigation of Potential Drug-drug Interactions Between Faldaprevir and the Immunosuppressant Drugs Cyclosporine or Tacrolimus

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 1 clinical and 1 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).