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DRUG:

lartesertib (M4076)

i
Other names: M4076, M-4076, M 4076
Associations
Company:
EMD Serono
Drug class:
ATM kinase inhibitor
Associations
4ms
Tuvusertib Combined With Niraparib or Lartesertib in Participants With Epithelial Ovarian Cancer (DDRiver EOC 302) (clinicaltrials.gov)
P2, N=60, Recruiting, EMD Serono Research & Development Institute, Inc. | Not yet recruiting --> Recruiting
Enrollment open • Combination therapy
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Zejula (niraparib) • tuvusertib (M1774) • lartesertib (M4076)
6ms
New P2 trial • Combination therapy
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Zejula (niraparib) • tuvusertib (M1774) • lartesertib (M4076)
8ms
Study of M1774 in Combination With DNA Damage Response Inhibitor or Immune Checkpoint Inhibitor (DDRiver Solid Tumors 320) (clinicaltrials.gov)
P1, N=72, Recruiting, EMD Serono Research & Development Institute, Inc. | Trial completion date: Dec 2023 --> May 2026 | Trial primary completion date: Dec 2023 --> Mar 2026
Trial completion date • Trial primary completion date • Combination therapy • Checkpoint inhibition • IO biomarker • Metastases
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Bavencio (avelumab) • tuvusertib (M1774) • lartesertib (M4076)
over1year
First-in-human Study of M4076 in Advanced Solid Tumors (DDRiver Solid Tumors 410) (clinicaltrials.gov)
P1, N=30, Completed, EMD Serono Research & Development Institute, Inc. | Active, not recruiting --> Completed
Trial completion • Metastases
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CHEK2 (Checkpoint kinase 2)
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lartesertib (M4076)
over1year
Selective inhibition of ATM-dependent double-strand break repair and checkpoint control synergistically enhances the efficacy of ATR inhibitors. (PubMed, Mol Cancer Ther)
In cancer cells with functional ATM and p53 signaling, selective suppression of ATR catalytic activity by M6620 induced G1-phase arrest to prevent S-phase entry with unrepaired DSBs. The selective ATM inhibitors, M3541 and M4076, suppressed both ATM-dependent cell-cycle checkpoints, and DSB repair lowered the p53 protective barrier and extended the life of ATR inhibitor-induced DSBs...ATM inhibitor synergistically potentiated the ATR inhibitor efficacy in cancer cells in vitro and increased ATR inhibitor efficacy in vivo at doses that did not show overt toxicities. Further, a combination study in 26 patient-derived xenograft models of triple negative breast cancer with the newer generation ATR inhibitor M4344 and ATM inhibitor M4076 demonstrated substantial improvement in efficacy and survival compared to single-agent M4344, suggesting a novel and potentially broad combination approach to cancer therapy.
Journal
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berzosertib (M6620) • M3541 • gartisertib (M4344) • lartesertib (M4076)
almost2years
First-in-human Study of M4076 in Advanced Solid Tumors (DDRiver Solid Tumors 410) (clinicaltrials.gov)
P1, N=30, Active, not recruiting, EMD Serono Research & Development Institute, Inc. | Recruiting --> Active, not recruiting
Enrollment closed • Metastases
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CHEK2 (Checkpoint kinase 2)
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lartesertib (M4076)
2years
First-in-human Study of M4076 in Advanced Solid Tumors (DDRiver Solid Tumors 410) (clinicaltrials.gov)
P1, N=30, Recruiting, EMD Serono Research & Development Institute, Inc. | Trial completion date: Aug 2022 --> May 2023 | Trial primary completion date: Aug 2022 --> May 2023
Trial completion date • Trial primary completion date
|
CHEK2 (Checkpoint kinase 2)
|
lartesertib (M4076)
over3years
First-in-human Study of M4076 in Advanced Solid Tumors (DDRiver Solid Tumors 410) (clinicaltrials.gov)
P1, N=30, Recruiting, EMD Serono Research & Development Institute, Inc. | Not yet recruiting --> Recruiting
Clinical • Enrollment open
|
CHEK2 (Checkpoint kinase 2)
|
lartesertib (M4076)
over3years
First-in-human Study of M4076 in Advanced Solid Tumors (DDRiver Solid Tumors 410) (clinicaltrials.gov)
P1, N=30, Not yet recruiting, EMD Serono Research & Development Institute, Inc.
Clinical • New P1 trial
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CHEK2 (Checkpoint kinase 2)
|
lartesertib (M4076)