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DRUG:

SLS009

i
Other names: SLS009, GFH009, GFH-009, GFH 009
Company:
GenFleet Therap, SELLAS Life Sciences
Drug class:
CDK9 inhibitor
6ms
Study of SLS009 (Formerly GFH009) a Potent Highly Selective CDK9 Inhibitor in Patients With Hematologic Malignancies (clinicaltrials.gov)
P1/2, N=160, Recruiting, Sellas Life Sciences Group | Trial completion date: Jun 2024 --> Dec 2025 | Trial primary completion date: Jun 2024 --> Jun 2025
Trial completion date • Trial primary completion date • Combination therapy
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Venclexta (venetoclax) • azacitidine • SLS009
7ms
New P1/2 trial • Combination therapy
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Brukinsa (zanubrutinib) • SLS009
9ms
A Study of GFH009 Monotherapy in Patients With Relapsed or Refractory Peripheral T-cell Lymphoma (PTCL) (clinicaltrials.gov)
P1/2, N=95, Recruiting, Zhejiang Genfleet Therapeutics Co., Ltd. | Not yet recruiting --> Recruiting
Enrollment open
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SLS009
11ms
The pharmacodynamic and mechanistic foundation for the antineoplastic effects of GFH009, a potent and highly selective CDK9 inhibitor for the treatment of hematologic malignancies. (PubMed, Oncotarget)
Through rapid 'on-off' CDK9 inhibition, GFH009 exerts a proapoptotic effect on HHM preclinical models triggered by dynamic deprivation of crucial cell survival signals. Our results mechanistically establish CDK9 as a targetable vulnerability in assorted HHMs and, along with the previously shown superior class kinome selectivity of GFH009 vs other CDK9 inhibitors, strongly support the rationale for currently ongoing clinical studies with this agent in acute myeloid leukemia and other HHMs.
PK/PD data • Journal
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MCL1 (Myeloid cell leukemia 1)
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MYC expression
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SLS009
over1year
New P1/2 trial
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SLS009
2years
First in Human (FIH) Study of GFH009, a Highly Selective Cyclin-Dependent Kinase 9 (CDK9) Inhibitor, in Patients with Relapsed/Refractory (r/r) Hematologic Malignancies (ASH 2022)
GFH009 as monotherapy is well tolerated at the tested doses and has shown clinical activity in patients with r/r lymphoma. The dose escalation in patients with AML and lymphoma is ongoing. Different dosing regimens are currently being explored for potentially better inhibition on the target.
Clinical • P1 data
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CDK9 (Cyclin Dependent Kinase 9)
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Venclexta (venetoclax) • SLS009
2years
In Vitro and In Vivo Studies Support GFH009, a Selective CDK9 Inhibitor, As a Potential Treatment for Hematologic Cancers (ASH 2022)
The reference compound enitociclib (BAY 1251152) was used for experimental validation. Although several cytotoxic molecules that inhibit CDK9 are in the therapeutic pipeline, many show cross-reactivity to other CDK family members, leading to toxicity and tolerability issues. GFH009 is a potent and highly selective CDK9 inhibitor with the ability to reduce expression of downstream oncogenes required for rapid cellular division and protein expression through specific, short-lived inhibition of CDK9. We postulate that this mechanism drives GFH009's inhibition of cellular division, as tumor stabilization and shrinkage appear to be dose-dependent.
Preclinical
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MCL1 (Myeloid cell leukemia 1) • CASP3 (Caspase 3)
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MYC expression • MCL1 expression
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enitociclib (VIP152) • SLS009
2years
AML-259 Pharmacokinetics and Bioequivalence of Two Formulations of GFH009 Maleate Injection in Sprague Dawley Rats. (PubMed, Clin Lymphoma Myeloma Leuk)
The PK profiles of GFH009 were comparable following single IV administration of two formulations of GFH009 maleate injection in SD rats, which supported application of the pH 6.0 formulation in Phase I trials in patients with relapsed/refractory hematologic conditions, including AML and lymphoma.
Clinical • PK/PD data • Preclinical • Journal
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MCL1 (Myeloid cell leukemia 1) • CDK9 (Cyclin Dependent Kinase 9)
|
MYC expression • MCL1 expression
|
SLS009
2years
Pharmacokinetics and Bioequivalence of Two Formulations of GFH009 Maleate Injection in Sprague Dawley Rats (SOHO 2022)
The PK profi les of GFH009 were comparable following single IV administration of two formulations of GFH009 maleate injection in SD rats, which supported application of the pH 6.0 formulation in Phase I trials in patients with relapsed/refractory hematologic conditions, including AML and lymphoma.
PK/PD data • Preclinical
|
MCL1 (Myeloid cell leukemia 1) • CDK9 (Cyclin Dependent Kinase 9)
|
MYC expression • MCL1 expression
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SLS009