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DRUG CLASS:

KAT6 inhibitor

11d
Dancing with KAT6A: Current advances and therapeutic potential in oncology of KAT6A inhibitors. (PubMed, Bioorg Chem)
PF-07248144 has shown antitumor activity in estrogen receptor-positive (ER+) breast cancer models and is currently undergoing clinical evaluation...This review provides a comprehensive overview of the structural and biological functions of KAT6A, its role in tumor progression, and the therapeutic potential of its inhibition. It summarizes the advancements in KAT6A inhibitor development from 2019 to the present, emphasizing the optimization processes from lead compounds to clinical candidates.
Review • Journal
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ER (Estrogen receptor) • KAT6A (Lysine Acetyltransferase 6A)
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ER positive
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prifetrastat (PF-07248144)
17d
Enrollment open
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itraconazole • prifetrastat (PF-07248144)
25d
A First-in-Human Study of MEN2312 in Adults With Advanced Breast Cancer (clinicaltrials.gov)
P1, N=240, Recruiting, Stemline Therapeutics, Inc. | Trial primary completion date: Oct 2025 --> Jun 2026
Trial primary completion date • First-in-human
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • AKT1 (V-akt murine thymoma viral oncogene homolog 1)
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Orserdu (elacestrant) • MEN2312
25d
New P2 trial • Tumor mutational burden
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
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ER positive • HER-2 negative • HER-2 mutation • HER-2 negative + ER positive
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fulvestrant • triptorelin • prifetrastat (PF-07248144)
26d
New P1 trial
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itraconazole • prifetrastat (PF-07248144)
4ms
A First-in-Human Study of MEN2312 in Adults With Advanced Breast Cancer (clinicaltrials.gov)
P1, N=240, Recruiting, Stemline Therapeutics, Inc. | N=124 --> 240
Enrollment change • First-in-human
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Orserdu (elacestrant) • MEN2312
5ms
Phase 1 Study of OP-3136 in Advanced or Metastatic Solid Tumors (clinicaltrials.gov)
P1, N=160, Recruiting, Olema Pharmaceuticals, Inc. | N=90 --> 160
Enrollment change • First-in-human
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fulvestrant
6ms
C4551001: Study of PF-07248144 in Advanced or Metastatic Solid Tumors (clinicaltrials.gov)
P1, N=320, Recruiting, Pfizer | Trial completion date: Jan 2028 --> Sep 2029
Trial completion date
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A)
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ER positive • HER-2 negative • HER-2 negative + ER positive
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Ibrance (palbociclib) • fulvestrant • letrozole • vepdegestrant (ARV-471) • atirmociclib (PF-07220060) • prifetrastat (PF-07248144)
6ms
A Study of KC1086 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
P1, N=66, Not yet recruiting, Beijing Konruns Pharmaceutical Co., Ltd.
New P1 trial
6ms
Enrollment open • Trial primary completion date
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everolimus • fulvestrant • exemestane • prifetrastat (PF-07248144)