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1m
SUMIT-BC: A Study of Samuraciclib in Combination With Fulvestrant in Metastatic or Locally Advanced Breast Cancer in Adult Participants (clinicaltrials.gov)
P2, N=60, Active, not recruiting, Carrick Therapeutics Limited | Recruiting --> Active, not recruiting
Enrollment closed • Combination therapy • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • TP53 (Tumor protein P53) • CDK4 (Cyclin-dependent kinase 4)
|
TP53 mutation • ER positive • HER-2 negative • HER-2 negative + ER positive
|
fulvestrant • samuraciclib (CT7001)
3ms
SUMIT-ELA: A Study of Samuraciclib and Elacestrant in Participants With Metastatic or Locally Advanced HR+/HER2-negative Breast Cancer (clinicaltrials.gov)
P1/2, N=49, Active, not recruiting, Carrick Therapeutics Limited | Recruiting --> Active, not recruiting
Enrollment closed • Combination therapy • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • TP53 (Tumor protein P53) • CDK4 (Cyclin-dependent kinase 4)
|
TP53 mutation • ER positive • HER-2 negative • ER mutation • ESR1 mutation • HER-2 negative + ER positive • HER-2 negative + ER positive + ESR1 mutation
|
Orserdu (elacestrant) • samuraciclib (CT7001)
7ms
P2 data • Metastases
|
CDK7 (Cyclin Dependent Kinase 7)
|
fulvestrant • samuraciclib (CT7001)
7ms
TACTIVE-U: A Study to Learn About the Study Medicine (Vepdegestrant) When Given With Other Medicines in People With Advanced or Metastatic Breast Cancer. (Sub-Study C) (clinicaltrials.gov)
P1/2, N=67, Recruiting, Pfizer | Trial completion date: Aug 2027 --> Jan 2027 | Trial primary completion date: Feb 2027 --> Jul 2026
Trial completion date • Trial primary completion date • Combination therapy • Metastases
|
vepdegestrant (ARV-471) • samuraciclib (CT7001)
8ms
TACTIVE-U: A Study to Learn About the Study Medicine (Vepdegestrant) When Given With Other Medicines in People With Advanced or Metastatic Breast Cancer. (Sub-Study C) (clinicaltrials.gov)
P1/2, N=67, Recruiting, Pfizer | Trial completion date: Feb 2027 --> Aug 2027 | Trial primary completion date: Aug 2026 --> Feb 2027
Trial completion date • Trial primary completion date • Combination therapy • Metastases
|
vepdegestrant (ARV-471) • samuraciclib (CT7001)
9ms
Phase classification • Combination therapy • Metastases
|
vepdegestrant (ARV-471) • samuraciclib (CT7001)
9ms
New P2 trial • Combination therapy • Metastases
|
vepdegestrant (ARV-471) • samuraciclib (CT7001)
10ms
Enrollment open
|
vepdegestrant (ARV-471) • samuraciclib (CT7001)
11ms
Phase classification
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • TP53 (Tumor protein P53) • CDK4 (Cyclin-dependent kinase 4)
|
TP53 mutation • ER positive • HER-2 negative • ER mutation • ESR1 mutation
|
Orserdu (elacestrant) • samuraciclib (CT7001)
11ms
New P1/2 trial
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • TP53 (Tumor protein P53) • CDK4 (Cyclin-dependent kinase 4)
|
TP53 mutation • ER positive • HER-2 negative • ER mutation • ESR1 mutation
|
Orserdu (elacestrant) • samuraciclib (CT7001)
almost1year
Active growth signaling promotes senescence and cancer cell sensitivity to CDK7 inhibition. (PubMed, Mol Cell)
We show that CDK7i, by samuraciclib, induces a permanent cell-cycle exit, known as senescence, without promoting DNA damage signaling or cell death...Reverting a growth-promoting mutation in PIK3CA to wild type decreases sensitivity to CDK7i. Our work establishes that enhanced growth alone promotes CDK7i sensitivity, providing an explanation for why some cancers are more sensitive to CDK inhibition than normally growing cells.
Journal
|
PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
|
PIK3CA mutation
|
samuraciclib (CT7001)
1year
SUMIT-ELA: Phase 1b/2 combination of cyclin-dependent kinase 7 inhibitor (CDK7i) samuraciclib and selective estrogen receptor degrader (SERD) elacestrant in advanced hormone receptor positive (HR+) breast cancer after CDK4/6i (SABCS 2023)
Samuraciclib (CT7001), a once daily oral CDK7 inhibitor has demonstrated a favorable safety profile and clinical activity in combination with fulvestrant (SERD) in patients with HR+/HER2- advanced breast cancer who have previously been treated with a CDK4/6 inhibitor [1]. Secondary endpoints are tolerability, clinical benefit response at 24 weeks, overall response rate, duration of response, best percent change in tumor size, pharmacokinetics and correlations between ctDNA detectable ESR1 and TP53 mutations and efficacy/safety finding in this patient population. The study opened for recruitment in June 2023.
P1/2 data • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • TP53 (Tumor protein P53) • CDK4 (Cyclin-dependent kinase 4) • CDK7 (Cyclin Dependent Kinase 7)
|
TP53 mutation • HR positive • HER-2 negative • ER mutation • ESR1 mutation
|
Guardant360® CDx
|
fulvestrant • Orserdu (elacestrant) • samuraciclib (CT7001)
1year
SUMIT-BC: Phase 2 randomized study of fulvestrant with or without the cyclin-dependent kinase 7 inhibitor (CDK7i) samuraciclib in advanced hormone receptor positive (HR+) breast cancer after CDK4/6i (SABCS 2023)
QoL and correlations between ctDNA detectable TP53 mutations and efficacy/safety finding in this patient population will be reported. The study opened for recruitment in June 2023.
P2 data • Clinical • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • TP53 (Tumor protein P53) • CDK4 (Cyclin-dependent kinase 4) • CDK7 (Cyclin Dependent Kinase 7)
|
TP53 mutation • HR positive • HER-2 negative
|
Guardant360® CDx
|
fulvestrant • samuraciclib (CT7001)
1year
TACTIVE-U: phase 1b/2 umbrella study of vepdegestrant, a PROteolysis TArgeting Chimera (PROTAC) estrogen receptor (ER) degrader, combined with other anticancer treatments in ER–positive advanced or metastatic breast cancer (SABCS 2023)
The cyclin-dependent kinase (CDK)4/6 inhibitors abemaciclib and ribociclib are approved in combination with an aromatase inhibitor or fulvestrant, or as monotherapy (abemaciclib), for ER+/HER2- advanced or metastatic breast cancer...Vepdegestrant is being evaluated in combination with abemaciclib (sub-study A; NCT05548127), ribociclib (sub-study B; NCT05573555), and samuraciclib (sub-study C)...The phase 2 portion of each sub-study will further evaluate the antitumor activity of the combinations; the primary endpoint is objective response and secondary endpoints include antitumor activity (CBR and DOR), PFS, overall survival, safety, plasma concentration of study drugs, and changes in circulating tumor DNA. Future combination sub-studies will be included in TACTIVE-U.
P1/2 data • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
|
ER positive • HER-2 negative
|
Verzenio (abemaciclib) • Kisqali (ribociclib) • fulvestrant • vepdegestrant (ARV-471) • samuraciclib (CT7001)
1year
Unraveling TIMP1: a multifaceted biomarker in colorectal cancer. (PubMed, Front Genet)
Drug sensitivity analysis, conducted using the DepMap database, revealed that colorectal cancer cell lines exhibiting elevated levels of TIMP1 expression were more responsive to certain drugs, such as CC-90003, Pitavastatin, Atuveciclib, and CT7001, compared to those with low levels of TIMP1. Furthermore, TIMP1 expression was positively correlated with that of ferroptosis-related genes, such as GPX4 and HSPA5. TIMP1 can be used as a biomarker for colorectal cancer and is associated with the immunological microenvironment, drug sensitivity, and ferroptosis inhibition in this disease.
Journal • IO biomarker
|
CXCL8 (Chemokine (C-X-C motif) ligand 8) • CXCL10 (Chemokine (C-X-C motif) ligand 10) • HAVCR2 (Hepatitis A Virus Cellular Receptor 2) • SPP1 (Secreted Phosphoprotein 1) • GPX4 (Glutathione Peroxidase 4) • TIMP1 (Tissue inhibitor of metalloproteinases 1) • HSPA5 (Heat Shock Protein Family A (Hsp70) Member 5) • MMP1 (Matrix metallopeptidase 1) • CXCL1 (Chemokine (C-X-C motif) ligand 1) • MMP3 (Matrix metallopeptidase 3)
|
TIMP1 overexpression • KIM1 expression • TIMP1 expression
|
samuraciclib (CT7001) • CC-90003 • atuveciclib (BAY 1143572) • pitavastatin
over1year
Disruption of CDK7 signaling leads to catastrophic chromosomal instability coupled with a loss of condensin-mediated chromatin compaction. (PubMed, J Biol Chem)
Notably, the regulation of condensin subunit gene expression is independent of super-enhancers. Together, these studies reveal a new role for CDK7 in sustaining chromatin configuration by ensuring the expression of condensin genes, including SMC2.
Journal
|
CDK7 (Cyclin Dependent Kinase 7)
|
samuraciclib (CT7001)
over1year
Dose escalation and expansion cohorts in patients with advanced breast cancer in a Phase I study of the CDK7-inhibitor samuraciclib. (PubMed, Nat Commun)
Here we report results from dose escalation and 2 expansion cohorts: Module 1A dose escalation with paired biopsy cohort in advanced solid tumor patients, Module 1B-1 triple negative breast cancer (TNBC) monotherapy expansion, and Module 2A fulvestrant combination in HR+/HER2- breast cancer patients post-CDK4/6-inhibitor. In this study, samuraciclib exhibits tolerable safety and PK is supportive of once-daily oral administration. Clinical activity in TNBC and HR+/HER2-breast cancer post-CDK4/6-inhibitor settings warrants further evaluation.
P1 data • Journal • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • TP53 (Tumor protein P53)
|
TP53 mutation • HER-2 negative
|
fulvestrant • samuraciclib (CT7001)
over1year
New P2 trial
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • TP53 (Tumor protein P53) • CDK4 (Cyclin-dependent kinase 4)
|
TP53 mutation • ER positive • HER-2 negative
|
fulvestrant • samuraciclib (CT7001)
over1year
The CDK7 inhibitor CT7001 (Samuraciclib) targets proliferation pathways to inhibit advanced prostate cancer. (PubMed, Br J Cancer)
This study supports CDK7 inhibition as a strategy to target deregulated cell proliferation and demonstrates CT7001 is a promising CRPC therapeutic, alone or in combination with AR-targeting compounds.
Journal • Metastases
|
Xtandi (enzalutamide capsule) • samuraciclib (CT7001)
over1year
TY-2699a is a highly potent CDK7 inhibitor to abolish dysfunctional tumor cell cycle for clinical development (AACR 2023)
Currently, trilaciclib, palbociclib, ribociclib, and abemaciclib that bear dual specificities against CDK4 and CDK6 have been approved for clinical usage, and more CDK4/6 targeted agents are actively under clinical evaluations, among which, TY-302, a novel CDK4/6 inhibitor being developed by TYK Medicines, is under Phase II trial (NCT04433494)...Several CDK7 targeted agents, such as SY-5609 and Samuraciclib (CT7001), are under development...# Shengli Dong and Apeng Liang contributed equally to this work. * Jun Li, Shengli Dong and Apeng Liang are the correspondent authors.
Clinical • Tumor cell
|
CCND1 (Cyclin D1) • CCNE1 (Cyclin E1) • CCNA2 (Cyclin A2) • CDK2 (Cyclin-dependent kinase 2) • CDK7 (Cyclin Dependent Kinase 7) • CDK1 (Cyclin-dependent kinase 1)
|
CDK7 overexpression
|
Ibrance (palbociclib) • Verzenio (abemaciclib) • Kisqali (ribociclib) • Cosela (trilaciclib) • SY-5609 • samuraciclib (CT7001) • TY-2699a • TY-302
almost2years
CT7001_001: Modular Study to Evaluate CT7001 Alone in Cancer Patients With Advanced Malignancies (clinicaltrials.gov)
P1/2, N=124, Completed, Carrick Therapeutics Limited | Active, not recruiting --> Completed
Trial completion • Combination therapy • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
|
fulvestrant • samuraciclib (CT7001)
2years
A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Participants With Breast Cancer (clinicaltrials.gov)
P1/2, N=510, Recruiting, Hoffmann-La Roche | Trial completion date: Apr 2027 --> Oct 2026 | Trial primary completion date: Oct 2026 --> Apr 2026
Trial completion date • Trial primary completion date
|
ER (Estrogen receptor) • CDK4 (Cyclin-dependent kinase 4)
|
HER-2 positive • ER positive
|
Herceptin (trastuzumab) • Tecentriq (atezolizumab) • Ibrance (palbociclib) • everolimus • Verzenio (abemaciclib) • Kisqali (ribociclib) • ipatasertib (RG7440) • Itovebi (inavolisib) • giredestrant (GDC-9545) • Pegasys (pegylated interferon α -2a) • Phesgo (pertuzumab/trastuzumab/hyaluronidase-zzxf) • samuraciclib (CT7001)
2years
CT7001_001: Modular Study to Evaluate CT7001 Alone in Cancer Patients With Advanced Malignancies (clinicaltrials.gov)
P1/2, N=124, Active, not recruiting, Carrick Therapeutics Limited | N=250 --> 124
Enrollment change • Combination therapy • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
|
fulvestrant • samuraciclib (CT7001)
almost3years
Clinical • Combination therapy
|
HER-2 (Human epidermal growth factor receptor 2) • CDK7 (Cyclin Dependent Kinase 7)
|
HER-2 positive • HR positive • HER-2 negative • HR positive + HER-2 negative
|
fulvestrant • samuraciclib (CT7001)
almost3years
Enrollment change
|
ER (Estrogen receptor) • CDK4 (Cyclin-dependent kinase 4)
|
HER-2 positive • ER positive
|
Herceptin (trastuzumab) • Ibrance (palbociclib) • everolimus • Verzenio (abemaciclib) • Kisqali (ribociclib) • ipatasertib (RG7440) • Itovebi (inavolisib) • giredestrant (GDC-9545) • Pegasys (pegylated interferon α -2a) • Phesgo (pertuzumab/trastuzumab/hyaluronidase-zzxf) • samuraciclib (CT7001)
3years
Study of samuraciclib (CT7001), a first-in-class, oral, selective inhibitor of CDK7, in combination with fulvestrant in patients with advanced hormone receptor positive HER2 negative breast cancer (HR+BC) (SABCS 2021)
Samuraciclib has demonstrated an acceptable safety profile with evidence of anti-tumour activity in combination with fulvestrant for patients with advanced HR+BC who have progressed on their prior CDK4/6i.
Clinical • Combination therapy
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • CDK7 (Cyclin Dependent Kinase 7)
|
HER-2 positive • HR positive • HER-2 negative • HR positive + HER-2 negative
|
fulvestrant • samuraciclib (CT7001)
3years
A clinical study of samuraciclib (CT7001), a first-in-class, oral, selective inhibitor of CDK7, in patients with advanced triple negative breast cancer (TNBC) (SABCS 2021)
Samuraciclib demonstrated an acceptable safety and tolerability profile with evidence of antitumour activity in advanced TNBC. References 1.Patel et al. ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment.
Clinical
|
CDK7 (Cyclin Dependent Kinase 7)
|
samuraciclib (CT7001)
3years
Clinical • Combination therapy
|
HER-2 (Human epidermal growth factor receptor 2) • CDK7 (Cyclin Dependent Kinase 7)
|
HER-2 positive • HR positive • HER-2 negative • HR positive + HER-2 negative
|
fulvestrant • samuraciclib (CT7001)
over3years
[VIRTUAL] Study of samuraciclib (CT7001), a first-in-class, oral, selective inhibitor of CDK7, in combination with fulvestrant in patients with advanced hormone receptor positive HER2 negative breast cancer (HR+BC) (ESMO 2021)
Samuraciclib has demonstrated an acceptable safety profile with evidence of anti-tumour activity in combination with fulvestrant for patients with advanced HR+BC who have progressed on their prior CDK4/6i.
Clinical • Combination therapy
|
HER-2 (Human epidermal growth factor receptor 2) • CDK7 (Cyclin Dependent Kinase 7)
|
HER-2 positive • HR positive • HER-2 negative • HR positive + HER-2 negative
|
fulvestrant • samuraciclib (CT7001)
over3years
Clinical • P1 data
|
ER (Estrogen receptor) • CDK7 (Cyclin Dependent Kinase 7)
|
samuraciclib (CT7001)
over3years
Modular Study to Evaluate CT7001 Alone in Cancer Patients With Advanced Malignancies (clinicaltrials.gov)
P1/2, N=250, Active, not recruiting, Carrick Therapeutics Limited | Recruiting --> Active, not recruiting | Trial completion date: Dec 2021 --> Mar 2023 | Trial primary completion date: Dec 2021 --> Mar 2023
Clinical • Enrollment closed • Trial completion date • Trial primary completion date • Combination therapy
|
HER-2 (Human epidermal growth factor receptor 2)
|
fulvestrant • samuraciclib (CT7001)