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    DRUG:

    rineterkib (LTT462)

    i
    Other names: LTT462, LTT 462, LTT-462, ERK-IN-1
    Company:
    Novartis
    Drug class:
    ERK2 inhibitor, ERK1 inhibitor
    Related drugs:
    22h
    A Study of Select Drug Combinations in Adult Patients With Advanced/Metastatic BRAF V600 Colorectal Cancer (clinicaltrials.gov)
    P1, N=122, Terminated, Novartis Pharmaceuticals | Trial completion date: Jan 2025 --> Sep 2024 | Active, not recruiting --> Terminated | Trial primary completion date: Jan 2025 --> Sep 2024; The decision of early termination was made due to business reasons, and was not based on any safety concerns for any of the treatment combinations.
    Trial completion date • Trial termination • Trial primary completion date
    |
    BRAF (B-raf proto-oncogene)
    |
    BRAF mutation • BRAF V600
    |
    Mekinist (trametinib) • Tafinlar (dabrafenib) • Tevimbra (tislelizumab-jsgr) • spartalizumab (PDR001) • naporafenib (ERAS-254) • batoprotafib (TNO155) • rineterkib (LTT462)
    1m
    A phase Ib study of the combination of naporafenib with rineterkib or trametinib in patients with advanced and metastatic KRAS- or BRAF-mutant non-small cell lung cancer. (PubMed, Lung Cancer)
    Both naporafenib combinations had acceptable safety profiles. Antitumor activity was limited in patients with NSCLC, despite the observed on-target pharmacodynamic effect.
    P1 data • Journal • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog) • DUSP6 (Dual specificity phosphatase 6)
    |
    KRAS mutation • BRAF mutation • NRAS mutation
    |
    Mekinist (trametinib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    1m
    Study of Efficacy and Safety of LXH254 Combinations in Patients With Previously Treated Unresectable or Metastatic Melanoma (clinicaltrials.gov)
    P2, N=134, Active, not recruiting, Novartis Pharmaceuticals | Trial primary completion date: Aug 2024 --> Nov 2024
    Trial primary completion date • Metastases
    |
    BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • BRAF V600
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    2ms
    ADORE: Platform Study of Novel Ruxolitinib Combinations in Myelofibrosis Patients (clinicaltrials.gov)
    P1/2, N=45, Completed, Novartis Pharmaceuticals | Active, not recruiting --> Completed
    Trial completion
    |
    Jakafi (ruxolitinib) • sabatolimab (MBG453) • rineterkib (LTT462) • siremadlin (HDM201) • Adakveo (crizanlizumab-tmca) • nisevokitug (NIS793)
    2ms
    A Study of Select Drug Combinations in Adult Patients With Advanced/Metastatic BRAF V600 Colorectal Cancer (clinicaltrials.gov)
    P1, N=122, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Oct 2024 --> Jan 2025 | Trial primary completion date: Oct 2024 --> Jan 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    BRAF (B-raf proto-oncogene)
    |
    BRAF mutation • BRAF V600
    |
    Mekinist (trametinib) • Tafinlar (dabrafenib) • Tevimbra (tislelizumab-jsgr) • spartalizumab (PDR001) • naporafenib (ERAS-254) • batoprotafib (TNO155) • rineterkib (LTT462)
    6ms
    A Phase Ib Study of LXH254-centric Combinations in NSCLC or Melanoma (clinicaltrials.gov)
    P1, N=241, Terminated, Novartis Pharmaceuticals | Active, not recruiting --> Terminated; Business reasons
    Trial termination • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    KRAS mutation • BRAF mutation • NRAS mutation
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    6ms
    Study of Efficacy and Safety of LXH254 Combinations in Patients With Previously Treated Unresectable or Metastatic Melanoma (clinicaltrials.gov)
    P2, N=134, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Apr 2024 --> Jul 2024
    Trial completion date • Metastases
    |
    BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • BRAF V600
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    9ms
    A Study of Select Drug Combinations in Adult Patients With Advanced/Metastatic BRAF V600 Colorectal Cancer (clinicaltrials.gov)
    P1, N=122, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: May 2024 --> Sep 2024 | Trial primary completion date: May 2024 --> Sep 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    BRAF (B-raf proto-oncogene)
    |
    BRAF mutation • BRAF V600
    |
    Mekinist (trametinib) • Tafinlar (dabrafenib) • Tevimbra (tislelizumab-jsgr) • spartalizumab (PDR001) • naporafenib (ERAS-254) • batoprotafib (TNO155) • rineterkib (LTT462)
    9ms
    ADORE: Platform Study of Novel Ruxolitinib Combinations in Myelofibrosis Patients (clinicaltrials.gov)
    P1/2, N=45, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Mar 2024 --> Jul 2024
    Trial completion date
    |
    Jakafi (ruxolitinib) • sabatolimab (MBG453) • rineterkib (LTT462) • siremadlin (HDM201) • Adakveo (crizanlizumab-tmca) • nisevokitug (NIS793)
    1year
    Study of Efficacy and Safety of LXH254 Combinations in Patients With Previously Treated Unresectable or Metastatic Melanoma (clinicaltrials.gov)
    P2, N=134, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Jan 2024 --> Apr 2024 | Trial primary completion date: Jan 2024 --> Apr 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • BRAF V600
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    1year
    A Phase Ib Study of LXH254-centric Combinations in NSCLC or Melanoma (clinicaltrials.gov)
    P1, N=242, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Dec 2023 --> Apr 2024 | Trial primary completion date: Dec 2023 --> Apr 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog) • DUSP6 (Dual specificity phosphatase 6)
    |
    KRAS mutation • BRAF mutation • NRAS mutation
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    over1year
    Study of Efficacy and Safety of LXH254 Combinations in Patients With Previously Treated Unresectable or Metastatic Melanoma (clinicaltrials.gov)
    P2, N=134, Active, not recruiting, Novartis Pharmaceuticals | Trial primary completion date: Oct 2023 --> Jan 2024
    Trial primary completion date • Metastases
    |
    BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • BRAF V600
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    over1year
    Study of Efficacy and Safety of LXH254 Combinations in Patients With Previously Treated Unresectable or Metastatic Melanoma (clinicaltrials.gov)
    P2, N=134, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Jul 2023 --> Oct 2023 | Trial primary completion date: May 2023 --> Oct 2023
    Trial completion date • Trial primary completion date • Metastases
    |
    BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • BRAF V600
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    over1year
    A Study of Select Drug Combinations in Adult Patients With Advanced/Metastatic BRAF V600 Colorectal Cancer (clinicaltrials.gov)
    P1, N=122, Active, not recruiting, Novartis Pharmaceuticals | Recruiting --> Active, not recruiting | N=350 --> 122
    Enrollment closed • Enrollment change • Metastases
    |
    BRAF (B-raf proto-oncogene) • DUSP6 (Dual specificity phosphatase 6)
    |
    BRAF mutation • BRAF V600
    |
    Mekinist (trametinib) • Tafinlar (dabrafenib) • Tevimbra (tislelizumab-jsgr) • spartalizumab (PDR001) • naporafenib (ERAS-254) • batoprotafib (TNO155) • rineterkib (LTT462)
    over1year
    A Phase Ib Study of LXH254-centric Combinations in NSCLC or Melanoma (clinicaltrials.gov)
    P1, N=242, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Jun 2023 --> Dec 2023 | Trial primary completion date: Jun 2023 --> Dec 2023
    Trial completion date • Trial primary completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog) • DUSP6 (Dual specificity phosphatase 6)
    |
    KRAS mutation • BRAF mutation • NRAS mutation
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    over1year
    A Study of Select Drug Combinations in Adult Patients With Advanced/Metastatic BRAF V600 Colorectal Cancer (clinicaltrials.gov)
    P1, N=350, Recruiting, Novartis Pharmaceuticals | Trial completion date: Oct 2024 --> Apr 2024 | Trial primary completion date: Oct 2024 --> Apr 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    BRAF (B-raf proto-oncogene) • DUSP6 (Dual specificity phosphatase 6)
    |
    BRAF mutation • BRAF V600
    |
    Mekinist (trametinib) • Tafinlar (dabrafenib) • Tevimbra (tislelizumab-jsgr) • spartalizumab (PDR001) • naporafenib (ERAS-254) • batoprotafib (TNO155) • rineterkib (LTT462)
    almost2years
    Study of Efficacy and Safety of LXH254 Combinations in Patients With Previously Treated Unresectable or Metastatic Melanoma (clinicaltrials.gov)
    P2, N=134, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Apr 2023 --> Jul 2023
    Trial completion date • Metastases
    |
    BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • BRAF V600
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    2years
    Study of Efficacy and Safety of LXH254 Combinations in Patients With Previously Treated Unresectable or Metastatic Melanoma (clinicaltrials.gov)
    P2, N=134, Active, not recruiting, Novartis Pharmaceuticals | Trial primary completion date: Aug 2022 --> Feb 2023
    Trial primary completion date
    |
    BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • BRAF V600
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    over2years
    Study of Efficacy and Safety of LXH254 Combinations in Patients With Previously Treated Unresectable or Metastatic Melanoma (clinicaltrials.gov)
    P2, N=134, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Oct 2022 --> Mar 2023
    Trial completion date
    |
    BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • BRAF V600
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    over2years
    A Phase Ib Study of LXH254-centric Combinations in NSCLC or Melanoma (clinicaltrials.gov)
    P1, N=241, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Nov 2022 --> Apr 2023 | Trial primary completion date: Nov 2022 --> Apr 2023
    Trial completion date • Trial primary completion date
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog) • DUSP6 (Dual specificity phosphatase 6)
    |
    KRAS mutation • BRAF mutation • NRAS mutation
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    over2years
    A Study of Select Drug Combinations in Adult Patients With Advanced/Metastatic BRAF V600 Colorectal Cancer (clinicaltrials.gov)
    P1, N=350, Recruiting, Novartis Pharmaceuticals | Trial completion date: Jun 2024 --> Oct 2024 | Trial primary completion date: Jun 2024 --> Oct 2024
    Trial completion date • Trial primary completion date
    |
    BRAF (B-raf proto-oncogene) • DUSP6 (Dual specificity phosphatase 6)
    |
    BRAF mutation • BRAF V600
    |
    Mekinist (trametinib) • Tafinlar (dabrafenib) • Tevimbra (tislelizumab-jsgr) • spartalizumab (PDR001) • naporafenib (ERAS-254) • batoprotafib (TNO155) • rineterkib (LTT462)
    over2years
    Study of Efficacy and Safety of LXH254 Combinations in Patients With Previously Treated Unresectable or Metastatic Melanoma (clinicaltrials.gov)
    P2, N=320, Recruiting, Novartis Pharmaceuticals | Trial completion date: Sep 2023 --> Oct 2022 | Trial primary completion date: Nov 2022 --> Aug 2022
    Trial completion date • Trial primary completion date
    |
    BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • BRAF V600
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    over2years
    A Study of Select Drug Combinations in Adult Patients With Advanced/Metastatic BRAF V600 Colorectal Cancer (clinicaltrials.gov)
    P1, N=350, Recruiting, Novartis Pharmaceuticals | Trial completion date: Aug 2023 --> Jun 2024 | Trial primary completion date: Aug 2023 --> Jun 2024
    Trial completion date • Trial primary completion date
    |
    BRAF (B-raf proto-oncogene) • DUSP6 (Dual specificity phosphatase 6)
    |
    BRAF mutation • BRAF V600
    |
    Mekinist (trametinib) • Tafinlar (dabrafenib) • Tevimbra (tislelizumab-jsgr) • spartalizumab (PDR001) • naporafenib (ERAS-254) • batoprotafib (TNO155) • rineterkib (LTT462)
    over2years
    A Phase Ib Study of LXH254-centric Combinations in NSCLC or Melanoma (clinicaltrials.gov)
    P1, N=241, Active, not recruiting, Novartis Pharmaceuticals | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog) • DUSP6 (Dual specificity phosphatase 6)
    |
    KRAS mutation • BRAF mutation • NRAS mutation
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    almost3years
    A Phase Ib Study of LXH254-centric Combinations in NSCLC or Melanoma (clinicaltrials.gov)
    P1, N=331, Recruiting, Novartis Pharmaceuticals | Trial primary completion date: Jan 2022 --> Nov 2022
    Trial primary completion date
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog) • DUSP6 (Dual specificity phosphatase 6)
    |
    KRAS mutation • BRAF mutation • NRAS mutation
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    almost3years
    Study of Efficacy and Safety of LXH254 Combinations in Patients With Previously Treated Unresectable or Metastatic Melanoma (clinicaltrials.gov)
    P2, N=320, Recruiting, Novartis Pharmaceuticals | Trial completion date: Apr 2023 --> Sep 2023
    Trial completion date
    |
    BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • BRAF V600
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    3years
    Adore: A Randomized, Open-Label, Phase 1/2 Open-Platform Study Evaluating Safety and Efficacy of Novel Ruxolitinib Combinations in Patients with Myelofibrosis (ASH 2021)
    Methods ADORE (NCT04097821) is a 3-part, open-label, multicenter, phase 1/2, platform study that will assess the safety and efficacy of RUX in combination with 5 novel compounds for the treatment of MF: siremadlin (HDM2 inhibitor), crizanlizumab (anti-P-selectin antibody), sabatolimab (anti-TIM-3 antibody), rineterkib (ERK1/2 inhibitor) and NIS793 (anti-TGFβ antibody) ( Figure ). Assuming all five combination treatments enter Part 2 and one combination treatment is expanded in Part 3, a total of 240 patients are planned to be enrolled. The study is open for enrolling into Part 1.
    Clinical • P1/2 data
    |
    MDM2 (E3 ubiquitin protein ligase) • TGFB1 (Transforming Growth Factor Beta 1)
    |
    Jakafi (ruxolitinib) • sabatolimab (MBG453) • rineterkib (LTT462) • siremadlin (HDM201) • Adakveo (crizanlizumab-tmca) • nisevokitug (NIS793)
    3years
    A Phase Ib Study of LXH254-centric Combinations in NSCLC or Melanoma (clinicaltrials.gov)
    P1, N=331, Recruiting, Novartis Pharmaceuticals | Trial completion date: May 2022 --> Nov 2022
    Clinical • Trial completion date
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog) • DUSP6 (Dual specificity phosphatase 6)
    |
    KRAS mutation • BRAF mutation • NRAS mutation
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    3years
    Study of Efficacy and Safety of LXH254 Combinations in Patients With Previously Treated Unresectable or Metastatic Melanoma (clinicaltrials.gov)
    P2, N=320, Recruiting, Novartis Pharmaceuticals | Trial primary completion date: Apr 2023 --> Nov 2022
    Clinical • Trial primary completion date
    |
    BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • BRAF V600
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    over3years
    A Study of Select Drug Combinations in Adult Patients With Advanced/Metastatic BRAF V600 Colorectal Cancer (clinicaltrials.gov)
    P1, N=395, Recruiting, Novartis Pharmaceuticals | N=280 --> 395 | Trial completion date: Feb 2023 --> Aug 2023 | Trial primary completion date: Feb 2023 --> Aug 2023
    Clinical • Enrollment change • Trial completion date • Trial primary completion date
    |
    BRAF (B-raf proto-oncogene) • DUSP6 (Dual specificity phosphatase 6)
    |
    BRAF mutation • BRAF V600
    |
    Mekinist (trametinib) • Tafinlar (dabrafenib) • spartalizumab (PDR001) • naporafenib (ERAS-254) • batoprotafib (TNO155) • rineterkib (LTT462)
    almost4years
    A Phase Ib Study of LXH254-centric Combinations in NSCLC or Melanoma (clinicaltrials.gov)
    P1, N=315, Recruiting, Novartis Pharmaceuticals | Trial completion date: Jan 2022 --> May 2022
    Clinical • Trial completion date
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog) • DUSP6 (Dual specificity phosphatase 6)
    |
    KRAS mutation • BRAF mutation • NRAS mutation
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    4years
    Study of Efficacy and Safety of LXH254 Combinations in Patients With Previously Treated Unresectable or Metastatic Melanoma (clinicaltrials.gov)
    P2, N=320, Recruiting, Novartis Pharmaceuticals | Not yet recruiting --> Recruiting
    Clinical • Enrollment open
    |
    BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • BRAF V600
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    over4years
    A Study of Select Drug Combinations in Adult Patients With Advanced/Metastatic BRAF V600 Colorectal Cancer (clinicaltrials.gov)
    P1, N=280, Recruiting, Novartis Pharmaceuticals | Not yet recruiting --> Recruiting
    Clinical • Enrollment open • PD(L)-1 Biomarker
    |
    BRAF (B-raf proto-oncogene) • DUSP6 (Dual specificity phosphatase 6)
    |
    BRAF mutation • BRAF V600
    |
    Mekinist (trametinib) • Tafinlar (dabrafenib) • spartalizumab (PDR001) • naporafenib (ERAS-254) • batoprotafib (TNO155) • rineterkib (LTT462)
    over4years
    [VIRTUAL] Phase Ib study of LXH254 + LTT462 in patients with KRAS- or BRAF-mutant NSCLC (ESMO 2020)
    Funding: Novartis Pharmaceuticals Corporation. Clinical trial identification: NCT02974725.
    Clinical • P1 data
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • RAF1 (Raf-1 Proto-Oncogene Serine/Threonine Kinase)
    |
    BRAF V600E • KRAS mutation • BRAF mutation • BRAF V600 • BRAF G466A • BRAF K601
    |
    naporafenib (ERAS-254) • rineterkib (LTT462)
    over4years
    Study of Efficacy and Safety of LXH254 Combinations in Patients With Previously Treated Unresectable or Metastatic Melanoma (clinicaltrials.gov)
    P2, N=320, Not yet recruiting, Novartis Pharmaceuticals
    Clinical • New P2 trial
    |
    BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • BRAF V600
    |
    Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)
    over4years
    [VIRTUAL] Phase Ib study of LXH254 + LTT462 in patients (pts) with KRAS- or BRAFmutant NSCLC. (ASCO 2020)
    No abstract available
    Clinical • P1 data
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    naporafenib (ERAS-254) • rineterkib (LTT462)
    over4years
    [VIRTUAL] Phase I dose-finding study of oral ERK1/2 inhibitor LTT462 in patients (pts) with advanced solid tumors harboring MAPK pathway alterations. (ASCO 2020)
    LTT462 is well tolerated. Limited clinical activity was reported with single agent LTT462; best overall response was SD. An ongoing study is investigating LTT462 in combination with the RAF inhibitor, LXH254, in NSCLC and melanoma.
    Clinical • P1 data
    |
    BRAF (B-raf proto-oncogene) • DUSP6 (Dual specificity phosphatase 6)
    |
    BRAF mutation • DUSP6 expression
    |
    naporafenib (ERAS-254) • rineterkib (LTT462)
    over4years
    A Study of Select Drug Combinations in Adult Patients With Advanced/Metastatic BRAF V600 Colorectal Cancer (clinicaltrials.gov)
    P1, N=280, Not yet recruiting, Novartis Pharmaceuticals
    Clinical • New P1 trial • PD(L)-1 Biomarker
    |
    BRAF (B-raf proto-oncogene) • DUSP6 (Dual specificity phosphatase 6)
    |
    BRAF mutation • BRAF V600
    |
    Mekinist (trametinib) • Tafinlar (dabrafenib) • spartalizumab (PDR001) • naporafenib (ERAS-254) • batoprotafib (TNO155) • rineterkib (LTT462)