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- || exarafenib (KIN-2787) / Pierre Fabre
Trial completion date, Trial primary completion date: A Study to Evaluate KIN-2787 in Participants With BRAF and/or NRAS Mutation Positive Solid Tumors (clinicaltrials.gov) - May 29, 2024
P1, N=400, Recruiting, Sponsor: Pierre Fabre Medicament
Trial completion date: Jun 2024 --> Dec 2025 | Trial primary completion date: Mar 2024 --> Dec 2024
- | exarafenib (KIN-2787) / Kinnate Biopharma
Journal: The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition. (Pubmed Central) - Jan 17, 2024
However, the discovery of a potent and selective inhibitor with biopharmaceutical properties suitable to sustain robust target inhibition in the clinical setting has proven challenging. Herein, we report the discovery of exarafenib (15), a highly potent and selective inhibitor that intercepts the RAF protein in the dimer compatible ?C-helix-IN conformation and demonstrates anti-tumor efficacy in preclinical models with BRAF class I, II, and III and NRAS alterations.
- || exarafenib (KIN-2787) / Pierre Fabre
Enrollment change: A Study to Evaluate KIN-2787 in Participants With BRAF and/or NRAS Mutation Positive Solid Tumors (clinicaltrials.gov) - Oct 10, 2023
P1, N=400, Recruiting, Sponsor: Kinnate Biopharma
Herein, we report the discovery of exarafenib (15), a highly potent and selective inhibitor that intercepts the RAF protein in the dimer compatible ?C-helix-IN conformation and demonstrates anti-tumor efficacy in preclinical models with BRAF class I, II, and III and NRAS alterations. N=262 --> 400
- ||||| exarafenib (KIN-2787) / Kinnate Biopharma
Clinical: WATCH: @AlexSpiraMDPhD shares new dose escalation data from the first-in-human Phase 1 KIN-2787 study of the pan-RAF inhibitor exarafenib in patients with BRAF-altered solid tumors or NRAS-mutant melanoma. #melsm #Oncology https://t.co/5PNRZzBpRn (Twitter) - Jun 29, 2023
- || exarafenib (KIN-2787) / Pierre Fabre
Enrollment change: A Study to Evaluate KIN-2787 in Participants With BRAF and/or NRAS Mutation Positive Solid Tumors (clinicaltrials.gov) - Apr 18, 2023
P1, N=262, Recruiting, Sponsor: Kinnate Biopharma
N=262 --> 400 N=155 --> 262
- exarafenib (KIN-2787) / Kinnate Biopharma
Exarafenib (KIN-2787) is a potent, selective pan-RAF inhibitor with activity in preclinical models of BRAF class II/III mutant and NRAS mutant melanoma (Section 15; Poster Board #5) - Mar 14, 2023 - Abstract #AACR2023AACR_7328;
P1
In addition to efficacy in BRAF mutant tumors, these data support use of exarafenib in combination therapy with MEK inhibitors in NRAS mutant melanoma. A Ph I dose escalation clinical trial evaluating the safety and efficacy of exarafenib in monotherapy and in combination with binimetinib is ongoing (NCT04913285).
- exarafenib (KIN-2787) / Kinnate Biopharma
Trials in progress: a global phase 1/1b clinical trial evaluating exarafenib (KIN-2787), a highly selective pan-RAF inhibitor, in adult patients with BRAF-altered solid tumors and NRAS mutant melanoma (Chapin Theater - Convention Center) - Mar 14, 2023 - Abstract #AACR2023AACR_5501;
P1
Exarafenib achieves therapeutically meaningful drug exposures and demonstrates promising tolerability & clinical activity in BRAF or NRAS alteration-driven solid tumors. Pt enrollment & exarafenib treatment at 300 mg bid continues.
- ||| KIN-2787 / Kinnate Biopharma
$KNTE opens off 20% after delaying KIN-2787 readout from Q3 to Q4 2022, and now to H1 2023. $DAWN $SWTX $BGNE $PFE $RHHBY $NVS, Fore Bio, Lutris Pharma etc (Twitter) - Oct 12, 2022
- KIN-2787 / Kinnate Biopharma
Antitumor activity of KIN-2787, a next-generation pan-RAF inhibitor, in combination with MEK inhibition in preclinical models of human NRAS mutant melanoma. () - Apr 28, 2022 - Abstract #ASCO2022ASCO_5277;
P1
Preclinical in vitro and in vivo studies using KIN-2787 in combination with binimetinib demonstrated significant combination benefit in NRAS mutant melanoma models. Taken together with its unique selectively, these data support use of KIN-2787 in combination therapy in this patient segment.
- || belvarafenib (HM95573) / Roche, KIN-2787 / Kinnate Biopharma
Did you ever try to get on a belvarafenib or KIN-2787 trial? (Twitter) - Apr 2, 2022
- KIN-2787 / Kinnate Biopharma
Design and rationale of a first in human (FIH) phase 1/1b study evaluating KIN-2787, a potent and highly selective pan-RAF inhibitor, in adult patients with BRAF- and NRAS-mutation positive solid tumors (Section 35) - Mar 9, 2022 - Abstract #AACR2022AACR_5895;
P1
Enrollment began in August 2022. Trial is open globally.
- KIN-2787 / Kinnate Biopharma
Antitumor activity of KIN-2787, a next-generation pan-RAF inhibitor, in preclinical models of human RAF/RAS mutant melanoma (Section 25) - Mar 9, 2022 - Abstract #AACR2022AACR_4717;
P1
Data supports KIN-2787 use in acquired BRAF dimer-dependent resistance to BRAF+MEK inhibitor therapy. A Phase I dose escalation and expansion clinical trial evaluating the safety and efficacy of KIN-2787 is ongoing (NCT04913285).
- ||||| KIN-2787 / Kinnate Biopharma
Clinical data: #TTLC22 Dr. @Tadashi_Manabe presents preclinical activity of KIN-2787, a pan-RAF inhibitor, in #BRAF altered cell lines. Showing promise in resistant cells and in different mutation classes (II and III remain an unmet need). Looking forward to seeing clinical data. (Twitter) - Feb 23, 2022
- KIN-2787 / Kinnate Biopharma
Antitumor Activity of KIN-2787, a Next-Generation pan-RAF Inhibitor, in Preclinical Models of Human BRAF-alteration Driven Non-small Cell Lung Cancer (NSCLC) ([VIRTUAL]) - Feb 4, 2022 - Abstract #IASLCTTLC2022IASLC_TTLC_139;
P1
While the RAF inhibitor dabrafenib is approved for treatment of BRAF Class I-altered NSCLC (in combination with trametinib), there are no RAF targeted therapies for treatment of NSCLC patients with tumors driven by BRAF Class II or Class III dimer-dependent alterations, likely contributing to the inferior clinical outcomes of these patients (Dagogo-Jack et al...In contrast to dabrafenib or vemurafenib, approved BRAF inhibitors with activity limited to Class I BRAF alterations, KIN-2787 was most active in Class II and Class III BRAF mutant NSCLC cells (EC50 median values 264 nM and 24 nM, respectively)...A Phase I dose-escalation and expansion clinical trial evaluating the safety and efficacy of KIN-2787 is actively enrolling (NCT04913285). Patients with advanced and metastatic solid tumors, including NSCLC patients, whose cancers are driven by BRAF Class I, II, or III alterations will receive KIN-2787 treatment on this study.
- || exarafenib (KIN-2787) / Pierre Fabre
Enrollment change: A Study to Evaluate KIN-2787 in Participants With BRAF and/or NRAS Mutation Positive Solid Tumors (clinicaltrials.gov) - Jan 28, 2022
P1, N=155, Recruiting, Sponsor: Kinnate Biopharma
Patients with advanced and metastatic solid tumors, including NSCLC patients, whose cancers are driven by BRAF Class I, II, or III alterations will receive KIN-2787 treatment on this study. N=115 --> 155
- KIN-2787 / Fount Therap
[VIRTUAL] Design and rationale of a first in human (FIH) Phase 1/1b study evaluating KIN-2787, a potent and highly selective pan-RAF inhibitor, in adult patients with BRAF mutation positive solid tumors () - Sep 30, 2021 - Abstract #AACRNCIEORTC2021AACR_NCI_EORTC_405;
- ||| exarafenib (KIN-2787) / Pierre Fabre
Enrollment open: A Study to Evaluate KIN-2787 in Participants With BRAF and/or NRAS Mutation Positive Solid Tumors (clinicaltrials.gov) - Jun 21, 2021
P1, N=115, Recruiting, Sponsor: Kinnate Biopharma
N=115 --> 155 Not yet recruiting --> Recruiting
- | exarafenib (KIN-2787) / Pierre Fabre
New P1 trial: A Study to Evaluate KIN-2787 in Participants With BRAF and/or NRAS Mutation Positive Solid Tumors (clinicaltrials.gov) - Jun 3, 2021
P1, N=115, Not yet recruiting, Sponsor: Kinnate Biopharma
- KIN-2787 / Fount Therap
[VIRTUAL] The next-generation pan-RAF inhibitor, KIN-2787, is active in class II and class III BRAF mutant models. () - Apr 28, 2021 - Abstract #ASCO2021ASCO_923;
KIN-2787 is a next-generation pan-RAF inhibitor with pronounced in vitro and in vivo activity against human cancers driven by Class II and III BRAF mutations . A phase 1 dose escalation and expansion clinical trial evaluating the safety and efficacy of KIN-2787 monotherapy in patients with advanced or metastatic solid tumors harboring BRAF gene alterations, including Class II and III mutations, is expected to initiate in 2021.