[Unlike ABT-450, on which Enanta is partnered with ABT, EDP-239 is wholly owned by Enanta, a small private company. Other companies with NS5A inhibitors for HCV include BMY, GSK, VRTX, and Presidio Pharma. (The NS5A program from AZN might no longer be active—see #msg-47300638.)]
›Enanta Nominates EDP-239 as Lead Development Candidate for NS5A HCV Inhibitor Program
Tuesday March 2, 2010, 9:30 am EST
WATERTOWN, Mass., March 2 /PRNewswire/ -- Enanta Pharmaceuticals, Inc. announced today the nomination of lead development candidate, EDP-239, from its NS5A hepatitis C virus (HCV) inhibitor program. EDP-239 has demonstrated picomolar potency against multiple genotypes of the virus and a preclinical pharmacokinetic profile amenable to once-a-day dosing.
"Our NS5A inhibitor program is well positioned to generate a pipeline of clinical candidates, and we are excited about further characterization of our various leads with distinct structural diversity," said Yat Sun Or, Ph.D., Senior Vice President and Chief Scientific Officer of Enanta Pharmaceuticals. "The NS5A program represents an important asset in our portfolio of HCV inhibitors, which additionally includes protease, polymerase, and cyclophilin inhibitors. We look forward to exploring combinations and potential synergies of EDP-239 with our broader HCV portfolio."
Enanta's NS5A program and intellectual property estate in the HCV field were derived from its internal drug discovery efforts. Enanta anticipates progressing into IND-enabling preclinical studies for EDP-239 with the goal of initiating clinical trials in 2011.
About Enanta
Enanta Pharmaceuticals is a research and development company that uses its novel chemistry approach and drug discovery capabilities to create best in class small molecule drugs in the infectious disease field. Enanta is developing novel protease, NS5A, polymerase, and cyclophilin-based inhibitors targeted against the Hepatitis C virus (HCV). Additionally, the Company has created a new class of macrolide antibiotics, called Bicyclolides, which overcomes bacterial resistance. Antibacterial focus areas include superbugs, respiratory tract infections, and intravenous and oral treatments for hospital and community MRSA. Enanta is a privately held company headquartered in Watertown, MA. Enanta's news releases and other information are available on the company's web site at www.enanta.com.‹
[New entries for Enanta’s EDP-239 and the unnamed NS5A inhibitor from IDIX; updated entries for ABT-450, ABT-333, and ABT-072; AZN’s A-831 moved to lowest grouping. Note: there are now sufficiently many NS5A inhibitors in development that I am no longer classifying these compounds as ones with a novel MoA.]
The following paragraphs are in descending order of likelihood of success. There is no claim of completeness in this compilation, i.e. paragraphs 2-6 do not necessarily mention all of the applicable drug candidates within a given grouping.
Please see #msg-42396728 for the distinction between a nucleoside and a nucleotide, and see #msg-43114117 for some historical perspective from the HIV arena.
1. The two leading protease inhibitors: Telaprevir (VRTX/JNJ; phase-3) and Boceprevir (MRK; phase-3). The Telaprevir program is further advanced, so let’s call Telaprevir and Boceprevir 1a and 1b, respectively. Both drugs have shown very impressive efficacy in phase-2 trials, although neither has a completely clean safety profile (see references below).
Telaprevir in the treatment-naïve setting: phase-3 program: #msg-27623529 (ADVANCE study), #msg-26228377 (both studies); phase-2b program: #msg-29019931 (PROVE-1/2 trials made simple), #msg-28746843 (PROVE-1/2 detailed results); C208 study of BID vs TID dosing: #msg-43114192.
Telaprevir in the second-line setting: phase-3 program (REALIZE study): #msg-32901932; phase-2 program: #msg-37316151 (PROVE-3 study), #msg-42965441 (‘107’ open-label extension for PROVE-1/2 failures).
Boceprevir in the treatment-naïve setting: phase-3 program (SPRINT-2 and RESPOND-2): #msg-29474929; phase-2b program: #msg-42086185 (AASLD 2009 abstract re SPRINT-1), #msg-37298987, (interim SPRINT-1 results at EASL 2009), #msg-37298085 (EPO usage), #msg-31190433 (Dew’s musings on SPRINT-1 data).
Boceprevir in the second-line setting: phase-3 (RESPOND-2) study: #msg-29474929.
2. Programs in phase-2b or later:BI 201335 (B-I; phase-2b), a protease inhibitor: #msg-42086185, #msg-33564560; Debio 025 (NVS/Debiopharm, phase-2b), a cyclophilin inhibitor: #msg-46432280; ITMN-191 a/k/a/ RG7227 (Roche/ITMN, phase-2b), a protease inhibitor: #msg-46797334, #msg-43666728 (Dew’s bearish take), #msg-43632598 (first report of liver tox), #msg-45340745 (phase-2b design change and delay), #msg-42016434, #msg-44330890 (phase-1b boosting with ritonavir), #msg-43185247 (INFORM-1 data from AASLD 2009); Locteron (Biolex; phase-2b), a long-acting interferon made in transgenic plants that may qualify for the 505b2 approval pathway: #msg-37298340 (phase-2a data from EASL 2009), #msg-37178496 (phase-2b design), #msg-40953698 (manufacturing agreement); RG7128 (Roche/VRUS; phase-2b), a nucleoside polymerase inhibitor: #msg-46762882 (phase-2b overview), #msg-43836489 (safety evaluation passes in first phase-2b in genotype-1/4), #msg-43185247 (INFORM-1 data from AASLD 2009); Zalbin a/k/a/ Albuferon/Joulferon (HGSI/NVS; BLA and MAA submitted): #msg-36140577 (phase-3 data), #msg-36254180 (lack of SPA!), #msg-34770426 (new trial with monthly dosing).
3. Programs in phase-1b/2a with an established MoA: ABT-072 (ABT, phase-2), a non-nucleoside polymerase inhibitor: #msg-47086871; #msg-47060142; ABT-333 (ABT, phase-2a), a nucleoside polymerase inhibitor: #msg-47060142, #msg-42098204; ABT-450 (ABT/Enanta, phase-2a), a protease inhibitor: #msg-47060142, #msg-35708745; ACH-1625 (ACHN;phase-1b), a protease inhibitor: #msg-45339022, #msg-44560695, #msg-44566075; ANA598 (ANDS, phase-2a), a non-nucleoside “palm” polymerase inhibitor: #msg-47053147, #msg-47098741, #msg-47087879, #msg-44645147 (interim phase-2a data), #msg-40064675 (musings on phase-1b data); BMS-650032 (BMY, phase-2a), a protease/NS3 inhibitor that’s being tested in an all-oral trial with BMS-790052: #msg-44700187, #msg-40361108; BMS-790052 (BMY, phase-2a), an NS5A inhibitor that’s being tested in an all-oral trial with BMS-650032: #msg-44700187, #msg-33270670; GS9190 (GILD; phase-2), a non-nucleoside polymerase inhibitor with QT-prolongation issues that GILD is testing in an all-oral combination with GILD’s newly disclosed protease inhibitor GS9256: #msg-46036072; IDX184 (IDIX; phase-2a), a nucleotide polymerase-inhibitor: #msg-47150426 (phase-2a data from 50mg qD cohort), #msg-39719159, (phase-1b monotherapy data), #msg-39720566, #msg-26915921 (MoA and how IDX184 is better than NM283); IFN-alpha-XL (FLML; phase-2a): #msg-44688995; IFN-Lambda (BMY/ZGEN; phase-2): #msg-34768182 (BMY partnership), #msg-43123220 (final phase-1b data), #msg-43360640 (start of phase-2); MK-7009 (MRK, phase-2a), a protease inhibitor: #msg-34337398, #msg-34335327; PSI-7977 (VRUS, phase-2a), a nucleotide polymerase inhibitor that’s a single-isomer version of PSI-7851: #msg-45735193 (start of phase-2a), #msg-40115833 (phase-1b data for PSI-7851); TMC435 f/k/a/ TMC435350 (Medivir/JNJ; phase-2b), a protease inhibitor: #msg-43361309 (overview of phase-2a/2b program at 2009 AASLD), #msg-37298740 (phase-2a data at EASL 2009), #msg-45415884 (2010 PK trial re hepatic impairment); VCH-222 (VRTX, phase-2), a non-nucleoside “thumb” polymerase inhibitor (acquired from ViroChem) being tested with Telaprevir+SoC as well as with Telaprevir alone: #msg-47242513, #msg-47189924.
4. Very-early-stage programs with an established MoA: ACH-2684 (ACHN, preclinical), a protease inhibitor: #msg-46160360; EDP-239 (Enanta, preclinical): an NS5A inhibitor: #msg-47301187; ‘hyperglycosylated’ interferon (Alios BioPharma, preclinical): #msg-35612425; IDX320 (IDIX, phase-1), a macrocyclic protease inhibitor: #msg-45598790); IDX375 (IDIX,phase-1), a non-nucleoside “palm” polymerase inhibitor: #msg-45350536; MK-3281 (MRK, phase-1), a non-nucleoside “thumb” polymerase inhibitor: #msg-42093301 (safety signal in AASLD 2009 abstract); PSI-938 and PSI-879 (VRUS, preclinical), a pair of purine-analog nucleotide prodrugs: #msg-39322313, #msg-42245955; an unnamed NS5A inhibitor (IDIX, preclinical): #msg-47110147; an unnamed NS5A inhibitor (GSK via Genelabs, status unknown): #msg-33209281, #msg-33211420; an unnamed NS5A inhibitor (VRTX via ViroChem, preclinical): #msg-36022752; an unnamed NS5A inhibitor (Presidio Pharma, status unknown): #msg-27791536.
5. Programs in phase-2 or earlier with a novel MoA: ACH-1095 (ACHN, preclinical), an NS4A inhibitor that GILD dropped while retaining the right to opt back in: #msg-41217537; AVL-181 (Avila Therapeutics, preclinical), a small-molecule drug that purportedly binds to an infected hepatocyte: #msg-47113598; CF-102 (Can-Fite, phase-1/2), a polymerase inhibitor that purportedly induces apoptosis: #msg-39588570; clemizole (Stanford University, preclinical), an NS4B inhibitor: #msg-39883747; CTI-1027 (Conatus, phase-2): #msg-46034554; GI-5005 (GlobeImmune, phase-2), an injectable immunomodulator: #msg-37298510; IL-7 (Cytheris, phase-1/2) an injectable immunomodulator: #msg-33152073; IMO-2125 (IDRA, phase-1), a TLR9 agonist: #msg-44746537; ITX5061 (iTherX, phase-2a), MoA unknown: #msg-35319690; MB11362 (Roche/MBRX, preclinical), MoA undisclosed: #msg-38456136; nitazoxanide (Romark/Chugai, phase-2): #msg-35738696; SCY-635 (Scynexis, phase-1b), a cyclophilin inhibitor: #msg-46669845; SD-101 (DVAX, phase-1b), a TLR9 agonist: #msg-45932364; SPC3649 (Santaris, preclinical), MoA based on microRNA: #msg-44177354; an unnamed entry inhibitor (PGNX, preclinical): #msg-38519885; an unnamed miR-122 inhibitor (GSK/Regulus, preclinical): #msg-47081015.
6. Programs on the back burner: A-831 (AZN, status unknown), an NS5A inhibitor: #msg-16682361 (acquisition), #msg-47300638 (possible termination); ANA773 (ANDS, phase-1), an oral TLR7 modulator that ANDS discontinued in Jun 2009 and is nominally available for partnering: #msg-38418158; SCH 900518/narlaprevir (MRK; phase-2a), a protease inhibitor originally owned by Schering-Plough that MRK discontinued following a pipeline pruning: #msg-47224801 (3/1/10 announcement of discontinuation), #msg-43169835 (interim phase-2a data), #msg-34338549 (final phase-1b data); taribavirin (VRX, phase-2b), a “legacy” prodrug of ribavirin that has been floating around for a long time: #msg-38280961 (musings on final phase-2b data), #msg-37299101 (detailed 60-week data); VX-813/VX-985 (VRTX, phase-1/preclinical), protease inhibitors that were previously touted as the backups to Telaprevir: #msg-45333927.
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