Turning Point Therapeutics Presents TRIDENT-1 Study Clinical Data for Repotrectinib in NTRK+ Advanced Solid Tumors in Plenary Session at 2021 AACR-NCI-EORTC Conference

On October 8, 2021 Turning Point Therapeutics, Inc. (NASDAQ: TPTX), a precision oncology company developing next-generation therapies that target genetic drivers of cancer, reported the presentation of early clinical data from the NTRK-positive TKI-naïve and TKI-pretreated advanced solid tumor cohorts (EXP-5 and EXP-6) of the ongoing TRIDENT-1 Phase 1/2 study of its lead drug candidate repotrectinib (Press release, Turning Point Therapeutics, OCT 8, 2021, View Source [SID1234591020]).

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These data are being presented today at a plenary session at the Virtual AACR-NCI-EORTC (Free AACR-NCI-EORTC Whitepaper) International Conference on Molecular Targets and Cancer Therapeutics (EORTC-NCI-AACR) (Free ASGCT Whitepaper) (Free EORTC-NCI-AACR Whitepaper) hosted by the American Association for Cancer Research (AACR) (Free AACR Whitepaper), the National Cancer Institute (NCI), and the European Organisation for Research and Treatment of Cancer (EORTC) being held October 7-10.

"These data in patients with NTRK-positive advanced solid tumors are encouraging and support further investigation of repotrectinib in this patient population, especially in the TKI-pretreated setting where there are no currently approved targeted therapies," said Mohammad Hirmand, M.D., chief medical officer. "Based on these findings and repotrectinib having recently been granted Breakthrough Therapy designation for NTRK-positive TKI-pretreated advanced solid tumors, we look forward to discussing next steps toward potential registration of repotrectinib in this patient population at a Type B meeting with the FDA anticipated in the first half of 2022."

Repotrectinib Early Data from Phase 1/2 TRIDENT-1 Study from NTRK-Positive Advanced Solid Tumor Cohorts (EXP-5, EXP-6)
The early Phase 2 TRIDENT-1 dataset utilizes an August 26, 2021 data cutoff. The safety analysis includes 301 treated patients from the pooled Phase 1 and Phase 2 portions of TRIDENT-1 across all cohorts, and the preliminary efficacy analysis includes 40 evaluable patients from the pooled Phase 1 and Phase 2 portions of TRIDENT-1 in the NTRK-positive advanced solid tumor cohorts (EXP-5, EXP-6). Of the 40 patients, 17 were TKI-naïve and 23 were TKI-pretreated. Phase 2 patients included in the efficacy analysis had baseline measurable disease and at least one post-baseline evaluable scan or were off treatment prior to first post-baseline scan. Responses were confirmed with a subsequent scan at least 28 days later per RECIST 1.1 and were determined by physician assessment for Phase 2 patients. Phase 1 patients included in the efficacy analysis were treated at or above the Phase 2 dose, with responses assessed by blinded independent central review (BICR). The Phase 1 data cutoff date was July 22, 2019 for responses and August 26, 2021 for duration of treatment.

The findings were reported in a pre-recorded oral plenary presentation by Benjamin Besse, M.D., Ph.D., professor of Medical Oncology at Paris-Saclay University and full-time cancer specialist at Gustave Roussy Cancer Center available on October 8 at 10:05 a.m. ET on the meeting website.

Pooled Phase 1 and Phase 2 Preliminary Efficacy Analysis (n=40)

In the NTRK-positive TKI-naïve advanced solid tumor population (EXP-5: n=17), the confirmed Objective Response Rate (cORR) was 41% (95% CI: 18-67). At the time of the data cutoff, three patients with limited time on treatment achieved stable disease with tumor regression of -21%, -23%, and -27% on their first post-baseline scans, and were awaiting their next scans. Duration of response ranged from 1.9+ to 7.4+ months, and the duration of treatment in the 17 patients ranged from 0.9 to 30.7+ months.

In the NTRK-positive TKI-pretreated advanced solid tumor population (EXP-6: n=23), the cORR was 48% (95% CI: 27-69). As of the cutoff date, three patients had unconfirmed partial responses (uPRs). Two uPRs have been confirmed since the cutoff date and are included in the cORR; the third patient with a uPR was on treatment awaiting a confirmatory scan and is not considered a responder in the cORR. The 48% cORR is an update since the pre-recorded presentation. Duration of response ranged from 0.9+ to 15.1 months, and the duration of treatment in the 23 patients ranged from 0.6 to 20.8 months.

Of the 23 NTRK-positive TKI-pretreated advanced solid tumor patients, 13 (57%) had NTRK solvent front mutations. In these 13 patients, the cORR was 62% (95% CI: 32-86) including one patient who had a complete response. As of the cutoff date, three patients had unconfirmed partial responses (uPRs). Two uPRs have been confirmed since the cutoff date and are included in the cORR; the third patient with a uPR was on treatment awaiting a confirmatory scan and is not considered a responder in the cORR. The 62% cORR is an update since the pre-recorded presentation. Duration of response ranged from 0.9+ to 13.7 months.
Preliminary Safety Analysis (n=301)

Repotrectinib was generally well tolerated.

The most frequently reported treatment-emergent adverse event (TEAE) was low-grade dizziness (60%) of which 76% of reported cases were grade 1. Eleven patients (4%) reported ataxia in the absence of dizziness. No events of dizziness or ataxia led to treatment discontinuation.

Dose modifications due to TEAEs included 27% of patients who had dose reduction and 11% who had drug discontinuation.
Turning Point also announced the publication of preclinical data of repotrectinib in the American Association of Cancer Research’s peer reviewed journal, Molecular Cancer Therapeutics. Preclinical studies described in the publication titled "Molecular Characteristics of Repotrectinib That Enable Potent Inhibition of TRK Fusion Proteins and Resistant Mutations" show that repotrectinib potently inhibited TRK fusion proteins and resistance mutations. Repotrectinib was the most potent inhibitor of wild-type TRKA/B/C fusions and was more potent than selitrectinib against all tested resistance mutations.

Repotrectinib was recently granted Breakthrough Therapy designation for the treatment of patients with advanced solid tumors that have an NTRK gene fusion who have progressed following treatment with one or two prior TRK tyrosine kinase inhibitors, with or without prior chemotherapy, and have no satisfactory alternative treatments. The company is planning to discuss next steps towards potential registration of repotrectinib in this patient population at a Type B meeting with the U.S. Food and Drug Administration (FDA) anticipated in the first half of 2022.

H3 Biomedicine Presents Update on Intratumoral E7766 Clinical Program for Advanced Solid Tumors or Lymphomas at AACR-NCI-EORTC Conference

On October 8, 2021 H3 Biomedicine Inc. (H3), a U.S.-based precision medicine research & development subsidiary of Eisai Co., Ltd., reported it will be providing an update on its intratumoral E7766 clinical program for advanced solid tumors or lymphomas in a poster presentation at the 2021 American Association for Cancer Research (AACR) (Free AACR Whitepaper), the National Cancer Institute, and the European Organisation for Research and Treatment of Cancer (AACR-NCI-EORTC) (Free AACR-NCI-EORTC Whitepaper) Virtual AACR-NCI-EORTC (Free AACR-NCI-EORTC Whitepaper) International Conference on Molecular Targets and Cancer Therapeutics (EORTC-NCI-AACR) (Free ASGCT Whitepaper) (Free EORTC-NCI-AACR Whitepaper) being held on October 7-10, 2021 (Press release, H3 Biomedicine, OCT 8, 2021, View Source [SID1234591019]).

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"Harnessing the innate immune response holds therapeutic promise but may require precision medicine approaches," said Antonio Gualberto, MD, PhD, Chief Medical Officer of H3. "Our studies show that genetic variants in the STING1 and TLR6-1-10 gene cluster are informative of upper aero digestive tract tumor patient prognosis and may uncover opportunities for therapeutic intervention. We continue to be encouraged by our ongoing clinical results with E7766 and we look forward to further advancing its Phase 1 dose escalation study."

Abstract Number: P110
Poster Title: Neandertal Introgressions Contribute to Upper Aero-Digestive Tract Tumor Patient Survival and Identify Patients who may Benefit from STING Agonist Treatment
Presenter: Antonio Gualberto, MD, PhD, H3 Biomedicine

About E7766
E7766 is a STING (Stimulator of Interferon Genes) agonist with broad specificity to all major genetic variants of human STING. Preclinical studies suggest that treatment with E7766 by intratumoral administration has anti-tumor activity at both local and systemic levels with induction of effective tumor-specific memory immune response. Intratumoral E7766 is currently being evaluated in a multicenter, phase 1/1b study to assess safety/tolerability and preliminary clinical activity of E7766 as a single agent administered intratumorally in participants with advanced solid tumors or lymphomas.

Exact Sciences schedules third quarter 2021 earnings call

On October 8, 2021 Exact Sciences Corp. (Nasdaq: EXAS) reported that the company plans to release its third quarter 2021 financial results after the close of the U.S. financial markets on November 2, 2021 (Press release, Exact Sciences, OCT 8, 2021, View Source [SID1234591017]). Following the release, company management will host a webcast and conference call at 5 p.m. ET to discuss financial results and business progress.

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An archive of the webcast will be available at www.exactsciences.com. A replay of the conference call will be available by calling 800-585-8367 domestically or 416-621-4642 internationally. The access code for the replay of the call is 2782364. The webcast, conference call and replay are open to all interested parties.

Mablink is present at BIO-Europe 2021

On October 8, 2021 Edouard LEROY Chief Business Officer of Mablink, reported that participates (digitally) in the next edition of the event BIO-Europe, held as a digital event from October 25 to 28, 2021 (Press release, Mablink Bioscience, OCT 8, 2021, View Source;utm_medium=rss&utm_campaign=mablink-is-present-at-bio-europe-2021 [SID1234591016]).

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BIO-Europe is one of the key events dedicated to partnering where global dealmakers meet to build partnerships and discuss investments opportunities.

Edouard will be available for bio-pharma companies, which would be interested in Mablink’s hydrophilic PSARlink ADC platforms or its assets that are available for partnering.

Repare Therapeutics Presents Preliminary Phase 1 Monotherapy Clinical Data from the Ongoing First-in-Human Phase 1/2 TRESR Study of RP-3500 in Solid Tumors at AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics

On October 8, 2021 Repare Therapeutics Inc. ("Repare" or the "Company") (Nasdaq: RPTX), a leading clinical-stage precision oncology company, reported the presentation of preliminary Phase 1 monotherapy clinical data from its Phase 1/2 TRESR (Treatment Enabled by SNIPRx) clinical trial of RP-3500, a potent and selective oral small molecule inhibitor of ATR (Ataxia-Telangiectasia and Rad3-related protein kinase) for the treatment of solid tumors with specific synthetic-lethal genomic alterations including those in the ATM gene (ataxia teleangectasia mutated kinase), at the AACR (Free AACR Whitepaper)-NCI-EORTC Virtual AACR-NCI-EORTC (Free AACR-NCI-EORTC Whitepaper) International Conference on Molecular Targets and Cancer Therapeutics (EORTC-NCI-AACR) (Free ASGCT Whitepaper) (Free EORTC-NCI-AACR Whitepaper) (Press release, Repare Therapeutics, OCT 8, 2021, View Source [SID1234591015]).

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The data are featured today at the AACR (Free AACR Whitepaper)-NCI-EORTC conference in an oral presentation titled, "First-in-Human biomarker-driven Phase I TRESR trial of ATR inhibitor RP-3500 in patients with advanced solid tumors harboring synthetic lethal genomic alterations" (Abstract number 4950). Preliminary data show that monotherapy RP-3500 is safe and well tolerated, with compelling early efficacy signals across multiple genotypes and tumor types in heavily pretreated patients.

The Company will subsequently host a virtual webcast event today, October 8th at 5:00 p.m. Eastern Time to discuss the latest results from the TRESR trial.

"Our initial data for 101 patients treated with RP-3500 in the ongoing TRESR study resulted in a firm recommendation for Phase 2 dose and schedule, suggest a favorable and differentiated safety profile and provide compelling early evidence of broad clinical efficacy across genotypes predicted by our SNIPRX platform," said Maria Koehler, MD, PhD, Chief Medical Officer of Repare. "The evolving nature of the data from this ongoing study and specifically the stable tolerability profile and maturing efficacy data offer a clear direction for further development of RP-3500. Additionally, we are excited to see that even at this early point in our clinical program, the pharmacokinetic and pharmacodynamic biomarker data already confirm proof-of-mechanism for RP-3500 in tumors with diverse molecular backgrounds."

"The TRESR study is the largest ever biomarker-selected trial testing single agent ATR inhibitor. We are very pleased that these data suggest RP-3500 may have a best-in-class profile as a potent and highly selective ATR inhibitor and represent compelling validation for the ability of our SNIPRx platform and our STEP2 process to improve efficacy through molecular selection of tumors," said Lloyd M. Segal, President and Chief Executive Officer of Repare. "We look forward to the imminent expansion of the TRESR study in a range of genotypes and, continuing and broadening our combination therapy studies, including with a range of PARP inhibitors and gemcitabine."

Key Initial Findings from the TRESR Phase 1/2 Study:

TRESR is a first-in-human, multi-center, open-label Phase 1/2 dose-escalation and expansion study, designed to establish the recommended Phase 2 dose and schedule, evaluate safety and pharmacokinetics and identify preliminary anti-tumor activity associated with RP-3500, given alone and in combination with talazoparib. The study also examined biomarker responses and their relationship with response to RP-3500 treatment.

Data presented in the abstract reflect the monotherapy cohort at data cutoff of June 4, 2021 and include 62 patients, while data presented at the conference reflect a data cutoff of August 15, 2021 and include 101 patients. Highlights from the data presented at the AACR (Free AACR Whitepaper)-NCI-EORTC conference include:

RP-3500 appears safe and well tolerated. The most common treatment emergent adverse events (TEAE) in any of the 101 patients treated, expectedly, was grade 1-2 anemia, with only 21.8% of all patients experiencing Grade 3 anemia (no Grade 4), and only 14.5% of those patients treated on the recommended weekly schedule of 3 days on/4 days off.
There were no discontinuations related to RP-3500 emergent adverse events and dose interruptions, reductions or red blood cell transfusions were infrequent on the recommended 3 days on/4 days off regimen.
Recommended Phase 2 dose (RP2D) and schedule for further monotherapy RP-3500 evaluation is 160mg, taken weekly for 3 days on and 4 days off. This schedule assures repeated weekly exposure to RP-3500 at an efficacious dose.
Antitumor activity was observed in patients with tumors harboring SNIPRX predicted genomic alternations at doses >100mg (ATM, CDK12, BRCA1, BRCA2, RAD51B, RAD51C, FZR1), across multiple tumor types and included patients after PARP inhibitor failure.
Meaningful clinical benefit was observed in 49% of 69 patients with available scans. Those include 12 patients with tumor responses per established international efficacy criteria, 14 patients with ongoing stable disease for at least 16 weeks and 8 patients with stable disease who only had two radiological evaluations, but had demonstrated significant decreases in tumor markers and tumor shrinkage of less than 30%.
Promising deep molecular responses in circulating tumor DNA (ctDNA) for tumors with STEP2 genomic alterations were observed in the initial set of patients available for serial ctDNA analysis
Company Virtual Webcast Event:

The Company will host a virtual investor webcast with accompanying slides for analysts and investors today at 5:00 p.m. Eastern Time to further discuss the RP-3500 data presented at the AACR (Free AACR Whitepaper)-NCI-EORTC Virtual AACR-NCI-EORTC (Free AACR-NCI-EORTC Whitepaper) International Conference on Molecular Targets and Cancer Therapeutics (EORTC-NCI-AACR) (Free ASGCT Whitepaper) (Free EORTC-NCI-AACR Whitepaper). Repare’s executive management team will be joined by Timothy Yap, MBBS, PhD, FRCP, Principal Investigator and Medical Director, Institute for Applied Cancer Science, Associate Professor, Department of Investigational Cancer Therapeutics, Division of Cancer Medicine, MD Anderson Cancer Center, Houston, Texas. At this event, the Company will provide an update on the status of the unconfirmed partial responses presented at the AACR (Free AACR Whitepaper)-NCI-EORTC conference since the August 15, 2021 data cutoff.

A live video webcast will be available in the Investor section of the Company’s website at View Source A webcast replay will also be archived for at least 30 days.

About Repare Therapeutics’ SNIPRx Platform

Repare’s SNIPRx platform is a genome-wide CRISPR-based screening approach that utilizes proprietary isogenic cell lines to identify novel and known synthetic lethal gene pairs and the corresponding patients who are most likely to benefit from the Company’s therapies based on the genetic profile of their tumors. Repare’s platform enables the development of precision therapeutics in patients whose tumors contain one or more genomic alterations identified by SNIPRx screening, in order to selectively target those tumors in patients most likely to achieve clinical benefit from resulting product candidates.