^
    Contact us  to learn more about
    our Premium Content:  News alerts, weekly reports and conference planners
    DRUG:

    taladegib (ENV 101)

    i
    Other names: ENV 101, LY-2940680, LY2940680, LY 2940680, ENV-IPF-101, ENV-ONC-101, ENV-101
    Associations

    News

    Trials
    Company:
    Eli Lilly, Endeavor BioMed
    Drug class:
    Hedgehog cell-signalling pathway inhibitor, SMO protein inhibitor
    Related drugs:
    Associations

    News

    Trials
    6ms
    A Phase 2 Trial of ENV-101 in Patients With Lung Fibrosis (WHISTLE-PF Trial) (clinicaltrials.gov)
    P2, N=320, Not yet recruiting, Endeavor Biomedicines, Inc.
    New P2 trial
    |
    taladegib (ENV 101)
    9ms
    A Study Evaluating the Safety and Efficacy of ENV-101 in Subjects With Idiopathic Pulmonary Fibrosis (IPF) (clinicaltrials.gov)
    P2, N=41, Completed, Endeavor Biomedicines, Inc. | Active, not recruiting --> Completed
    Trial completion
    |
    taladegib (ENV 101)
    11ms
    A Study Evaluating the Safety and Efficacy of ENV-101 (Taladegib) in Patients With Advanced Solid Tumors Harboring PTCH1 Loss of Function Mutations (clinicaltrials.gov)
    P2, N=44, Active, not recruiting, Endeavor Biomedicines, Inc. | Recruiting --> Active, not recruiting
    Enrollment closed • Metastases
    |
    PTCH1 (Patched 1)
    |
    PTCH1 mutation
    |
    taladegib (ENV 101)
    11ms
    A Study Evaluating the Safety and Efficacy of ENV-101 in Subjects With Idiopathic Pulmonary Fibrosis (IPF) (clinicaltrials.gov)
    P2, N=40, Active, not recruiting, Endeavor Biomedicines, Inc. | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    taladegib (ENV 101)
    1year
    Metastatic Basal Cell Carcinoma: Treatment with a potentially best in class Hedgehog Inhibitor, Taladegib (EADV 2023)
    Patient was further treated by vismodegib for 12 months followed by Cemiplimab. For the first time we report here that mBCC patients who were refractory to current standard of care treatments responded to taladegib with a duration of response of around one year with fewer and manageable adverse effects.
    PD(L)-1 Biomarker • IO biomarker • Metastases
    |
    PTCH1 (Patched 1)
    |
    PTCH1 mutation
    |
    Libtayo (cemiplimab-rwlc) • Erivedge (vismodegib) • taladegib (ENV 101)
    over2years
    A phase II study evaluating the safety and efficacy of ENV-101 (taladegib) in patients with advanced solid tumors harboring PTCH1 loss of function mutations (ESMO 2022)
    Stage 1 (phase IIa) of this protocol will enroll a total of 44 patients randomized between two dose levels. In the presence of acceptable efficacy, stage 2 (phase IIb) of this protocol will expand enrollment using a single dose level.
    Clinical • P2 data
    |
    PTCH1 (Patched 1) • SMO (Smoothened Frizzled Class Receptor)
    |
    PTCH1 mutation • SMO mutation
    |
    taladegib (ENV 101)
    over2years
    A Study Evaluating the Safety and Efficacy of ENV-101 (Taladegib) in Patients With Advanced Solid Tumors Harboring PTCH1 Loss of Function Mutations (clinicaltrials.gov)
    P2, N=44, Recruiting, Endeavor Biomedicines, Inc. | Not yet recruiting --> Recruiting | Initiation date: Jan 2022 --> May 2022
    Enrollment open • Trial initiation date
    |
    PTCH1 (Patched 1) • GLI1 (GLI Family Zinc Finger 1)
    |
    PTCH1 mutation
    |
    taladegib (ENV 101)
    almost3years
    A Study Evaluating the Safety and Efficacy of ENV-101 (Taladegib) in Patients With Advanced Solid Tumors Harboring PTCH1 Loss of Function Mutations (clinicaltrials.gov)
    P2, N=44, Not yet recruiting, Endeavor Biomedicines, Inc.
    New P2 trial
    |
    PTCH1 (Patched 1) • GLI1 (GLI Family Zinc Finger 1)
    |
    PTCH1 mutation
    |
    taladegib (ENV 101)
    almost3years
    Responses to LY2940680 in ovarian cancer cell lines demonstrate Hedgehog and WNT pathways crosstalk as potential biomarkers in clinical trials. (NCRI 2021)
    The value of these WNT pathway genes as predictive biomarkers of patient response to Hh inhibitors warrants further investigation. Impact statement Investigating crosstalk between Hh and WNT pathways could potentially lead to new therapies.
    Preclinical
    |
    GLI1 (GLI Family Zinc Finger 1) • MMP7 (Matrix metallopeptidase 7)
    |
    GLI1 expression
    |
    taladegib (ENV 101)
    over3years
    A phase 1b study of the Notch inhibitor crenigacestat (LY3039478) in combination with other anticancer target agents (taladegib, LY3023414, or abemaciclib) in patients with advanced or metastatic solid tumors. (PubMed, Invest New Drugs)
    The primary objective was to determine the recommended Phase 2 dose of crenigacestat in combination with other anticancer agents (taladegib, LY3023414 [dual inhibitor of phosphoinositide 3-kinase; mechanistic target of rapamycin], or abemaciclib). This study demonstrated that crenigacestat combined with different anticancer agents (taladegib, LY3023414, or abemaciclib) was poorly tolerated, leading to lowered dosing and disappointing clinical activity in patients with advanced or metastatic solid tumors. NCT02784795 and date of registration: May 27, 2016.
    Clinical • P1 data • Journal • Combination therapy
    |
    mTOR (Mechanistic target of rapamycin kinase)
    |
    Verzenio (abemaciclib) • sirolimus • samotolisib (LY3023414) • crenigacestat (LY3039478) • taladegib (ENV 101)
    over4years
    Taladegib controls early chondrocyte hypertrophy via inhibiting smoothened/Gli1 pathway. (PubMed, Am J Transl Res)
    Our results reveal Taladegib as a novel drug in controlling chondrocyte hypertrophy depending on Smo blocking, which plays a vital role in the homeostasis of cartilage and the development of OA. Besides, we found that Taladegib only works in the previous stage of chondrocytes hypertrophy but not in the later of the process.
    Journal
    |
    GLI1 (GLI Family Zinc Finger 1)
    |
    taladegib (ENV 101)