Seagen Highlights TUKYSA® (tucatinib) Data in Breast Cancer at Virtual 2020 San Antonio Breast Cancer Symposium

On December 8, 2020 Seagen Inc. (Nasdaq:SGEN) reported the presentation of new data from TUKYSA (tucatinib), its HER2-positive metastatic breast cancer therapy, at the San Antonio Breast Cancer Symposium (SABCS) Virtual Symposium, taking place December 8-11, 2020 (Press release, Seagen, DEC 8, 2020, View Source [SID1234572426]). Nine abstracts – including two spotlight posters – highlight the company’s commitment to addressing unmet needs in breast cancer.

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"Following this year’s FDA approval of TUKYSA, we continue to broadly study if more patients may benefit from this important medicine," said Roger Dansey, M.D., Chief Medical Officer at Seagen. "Data presented at the meeting from the HER2CLIMB trial demonstrate TUKYSA’s efficacy regardless of patients’ hormone receptor status, while other clinical and preclinical findings provide new insights about TUKYSA’s potential to help patients living with HER2-positive metastatic breast cancer."

Highlights for key data presentations at the meeting include:

Efficacy Outcomes by Hormone Receptor Status from HER2CLIMB Trial

Outcomes for TUKYSA (tucatinib) in combination with trastuzumab and capecitabine in patients with HER2-positive metastatic breast cancer from the pivotal HER2CLIMB trial by hormone receptor (HR) status will be featured in a spotlight poster (Abstract #PD3-08). Results will be presented by Erika P. Hamilton, M.D., Director, Breast Cancer and Gynecologic Cancer Research Program at the Sarah Cannon Research Institute.

As previously reported, the addition of TUKYSA to trastuzumab and capecitabine resulted in clinically meaningful improvements in overall survival (OS), progression-free survival (PFS) and objective response rate (ORR) compared to the addition of placebo. The new exploratory analyses presented at SABCS demonstrated that the PFS, OS and ORR improvements with TUKYSA were observed consistently across hormone receptor status subgroups, including in patients with brain metastases.

SABCS 2020 Data Presentations for Seagen Medicines and Pipeline Agents:

Below are presentation details related to TUKYSA and the investigational agent ladiratuzumab vedotin at SABCS. Published abstracts can be found here. Poster presentations will be available on December 9, 2020.

Abstract Title

Abstract No.

Presentation
Type / Date

Presenter

Tucatinib versus placebo in combination with trastuzumab and capecitabine for patients with locally advanced unresectable or HER2-positive metastatic breast cancer (HER2CLIMB): outcomes by hormone receptor status

#PD3-08

Spotlight Poster Discussion 3 – Wednesday, Dec. 9 from 6:45 – 7:45 p.m. CT

E. Hamilton

Impact of tucatinib on health-related quality of life in patients with HER2+ metastatic breast cancer with stable and active brain metastases

#PD13-04

Spotlight Poster Discussion 13 – Friday, Dec. 11 from 1 – 2:15 p.m. CT

A. Wardley

Tucatinib favourably modulates the immune microenvironment and synergises with anti-PD1 therapy in a trastuzumab resistant HER2+ murine model

#PS10-04

Poster Session 10 / Wednesday, Dec. 9 at 8 a.m. CT

R. Li

Tucatinib potentiates the activity of the antibody-drug conjugate T-DM1 in preclinical models of HER2-positive breast cancer

#PS10-08

Poster Session 10 / Wednesday, Dec. 9 at 8 a.m. CT

A. Kulukian

Real world treatment patterns and healthcare resource utilization among HER2+ metastatic breast cancer patients with and without brain metastases: a retrospective cohort study

#PS14-15

Poster Session 14 / Wednesday, Dec. 9 at 8 a.m. CT

C. Ike

Interim safety and efficacy analysis of phase IB/II clinical trial of tucatinib, palbociclib and letrozole in patients with hormone receptor and HER2-positive metastatic breast cancer

#PS10-03

Poster Session 10 / Wednesday, Dec. 9 at 8 a.m. CT

E. Shagisultanova

Trials-in-Progress

HER2CLIMB-02: A randomized, double-blind, phase 3 study of tucatinib or placebo with T-DM1 for unresectable locally-advanced or metastatic HER2+ breast cancer

#OT-28-01

Ongoing Trials Posters / Wednesday, Dec. 9 at 8 a.m. CT

S. Hurvitz

SGNLVA-001: a phase 1 open-label dose escalation and expansion study of SGN-LIV1A administered weekly in breast cancer

#OT-03-03

Ongoing Trials Posters / Wednesday, Dec. 9 at 8 a.m. CT

H.C. Beckwith

About TUKYSA (tucatinib)

TUKYSA is an oral medicine that is a tyrosine kinase inhibitor of the HER2 protein. In vitro (in lab studies), TUKYSA inhibited phosphorylation of HER2 and HER3, resulting in inhibition of downstream MAPK and AKT signaling and cell growth (proliferation), and showed anti-tumor activity in HER2-expressing tumor cells. In vivo (in living organisms), TUKYSA inhibited the growth of HER2-expressing tumors. The combination of TUKYSA and the anti-HER2 antibody trastuzumab showed increased anti-tumor activity in vitro and in vivo compared to either medicine alone. In the U.S., TUKYSA is approved in combination with trastuzumab and capecitabine for adult patients with advanced unresectable or metastatic HER2-positive breast cancer, including patients with brain metastases (disease that has spread to the brain), who have received one or more prior anti-HER2-based regimens in the metastatic setting. TUKYSA is approved in the U.S., Switzerland, Canada, Singapore and Australia and is under review in the European Union. As part of a strategic collaboration announced in September 2020 with Merck, known as MSD outside the United States and Canada, Merck has exclusive rights to commercialize TUKYSA in Asia, the Middle East and Latin America and other regions outside of the U.S., Canada and Europe.

U.S. Important Safety Information

Warnings and Precautions

Diarrhea – TUKYSA can cause severe diarrhea including dehydration, hypotension, acute kidney injury, and death. In HER2CLIMB, 81% of patients who received TUKYSA experienced diarrhea, including 12% with Grade 3 diarrhea and 0.5% with Grade 4 diarrhea. Both patients who developed Grade 4 diarrhea subsequently died, with diarrhea as a contributor to death. The median time to onset of the first episode of diarrhea was 12 days and the median time to resolution was 8 days. Diarrhea led to dose reductions of TUKYSA in 6% of patients and discontinuation of TUKYSA in 1% of patients. Prophylactic use of antidiarrheal treatment was not required on HER2CLIMB.

If diarrhea occurs, administer antidiarrheal treatment as clinically indicated. Perform diagnostic tests as clinically indicated to exclude other causes of diarrhea. Based on the severity of the diarrhea, interrupt dose, then dose reduce or permanently discontinue TUKYSA.
Hepatotoxicity – TUKYSA can cause severe hepatotoxicity. In HER2CLIMB, 8% of patients who received TUKYSA had an ALT increase >5 × ULN, 6% had an AST increase >5 × ULN, and 1.5% had a bilirubin increase >3 × ULN (Grade ≥3). Hepatotoxicity led to dose reduction of TUKYSA in 8% of patients and discontinuation of TUKYSA in 1.5% of patients.

Monitor ALT, AST, and bilirubin prior to starting TUKYSA, every 3 weeks during treatment, and as clinically indicated. Based on the severity of hepatotoxicity, interrupt dose, then dose reduce or permanently discontinue TUKYSA.
Embryo-Fetal Toxicity – TUKYSA can cause fetal harm. Advise pregnant women and females of reproductive potential risk to a fetus. Advise females of reproductive potential, and male patients with female partners of reproductive potential, to use effective contraception during TUKYSA treatment and for at least 1 week after the last dose.
Adverse Reactions

Serious adverse reactions occurred in 26% of patients who received TUKYSA. Serious adverse reactions in ≥2% of patients who received TUKYSA were diarrhea (4%), vomiting (2.5%), nausea (2%), abdominal pain (2%), and seizure (2%). Fatal adverse reactions occurred in 2% of patients who received TUKYSA including sudden death, sepsis, dehydration, and cardiogenic shock.

Adverse reactions led to treatment discontinuation in 6% of patients who received TUKYSA; those occurring in ≥1% of patients were hepatotoxicity (1.5%) and diarrhea (1%). Adverse reactions led to dose reduction in 21% of patients who received TUKYSA; those occurring in ≥2% of patients were hepatotoxicity (8%) and diarrhea (6%).

The most common adverse reactions in patients who received TUKYSA (≥20%) were diarrhea, palmar-plantar erythrodysesthesia, nausea, fatigue, hepatotoxicity, vomiting, stomatitis, decreased appetite, abdominal pain, headache, anemia, and rash.

Lab Abnormalities

In HER2CLIMB, Grade ≥3 laboratory abnormalities reported in ≥5% of patients who received TUKYSA were: decreased phosphate, increased ALT, decreased potassium, and increased AST. The mean increase in serum creatinine was 32% within the first 21 days of treatment with TUKYSA. The serum creatinine increases persisted throughout treatment and were reversible upon treatment completion. Consider alternative markers of renal function if persistent elevations in serum creatinine are observed.

Drug Interactions

Strong CYP3A or Moderate CYP2C8 Inducers: Concomitant use may decrease TUKYSA activity. Avoid concomitant use of TUKYSA.
Strong or Moderate CYP2C8 Inhibitors: Concomitant use of TUKYSA with a strong CYP2C8 inhibitor may increase the risk of TUKYSA toxicity; avoid concomitant use. Increase monitoring for TUKYSA toxicity with moderate CYP2C8 inhibitors.
CYP3A Substrates: Concomitant use may increase the toxicity associated with a CYP3A substrate. Avoid concomitant use of TUKYSA where minimal concentration changes may lead to serious or life-threatening toxicities. If concomitant use is unavoidable, decrease the CYP3A substrate dosage.
P-gp Substrates: Concomitant use may increase the toxicity associated with a P-gp substrate. Consider reducing the dosage of P-gp substrates where minimal concentration changes may lead to serious or life-threatening toxicity.
Use in Specific Populations

Lactation: Advise women not to breastfeed while taking TUKYSA and for at least 1 week after the last dose.
Renal Impairment: Use of TUKYSA in combination with capecitabine and trastuzumab is not recommended in patients with severe renal impairment (CLcr < 30 mL/min), because capecitabine is contraindicated in patients with severe renal impairment.
Hepatic Impairment: Reduce the dose of TUKYSA for patients with severe (Child-Pugh C) hepatic impairment.

Plus Therapeutics to Present at 13th Annual LD Micro Main Event Conference

On December 8, 2020 Plus Therapeutics, Inc. (Nasdaq: PSTV) (the "Company"), a clinical-stage company focused on making a positive impact on patients’ lives, reported that Marc Hedrick, M.D., President and Chief Executive Officer of Plus Therapeutics, has been invited to present a Company overview during the 13th Annual LD Micro Main Event Conference on Monday, December 14th at 10:40 a.m. ET (Press release, PLUS THERAPEUTICS, DEC 8, 2020, View Source [SID1234572404]).

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For conference participants, a live webcast of the presentation can be found by visiting the home page of the event at View Source A subsequent archived recording of the Company’s presentation will be available under the ‘Events’ tab of the Investor Relations section of the Plus Therapeutics website at www.plustherapeutics.com.

Corporate Presentation

On December 8, 2020 Curis, Inc. presented the corporate presentation (Presentation, Curis, DEC 8, 2020, View Source [SID1234572403]).

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H3 Biomedicine, Inc. Presents Data Update on H3B-6545 for Treatment of Locally Advanced or Metastatic Estrogen Receptor-positive, HER2-negative Breast Cancer at San Antonio Breast Cancer Symposium

On December 8, 2020 H3 Biomedicine, Inc. (H3), a U.S.-based precision medicine research & development subsidiary of Eisai Co., Ltd., reported the presentation of three posters at the 2020 San Antonio Breast Cancer Symposium (SABCS) (Press release, H3 Biomedicine, DEC 8, 2020, View Source [SID1234572402]). The presentations include interim data from H3’s ongoing Phase 1/2 clinical development program, H3B-6545, a potential first-in-class, orally available Selective ERα Covalent Antagonist (SERCA), in women with ER-positive, HER2-negative breast cancer.
"Our ongoing evaluation of H3B-6545 underscores our mission to work to develop new oncology therapeutics by unlocking cancer genomics, real-world patient data and biomarkers," said Antonio Gualberto, MD, PhD, Chief Medical Officer of H3. "H3B-6545 is part of a new class of endocrine therapies that target normal or mutated versions of the ER-alpha protein and we look forward to showcasing its progress and potential at SABCS 2020."

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H3B-6545 PRESENTATIONS

Abstract Number: 1142
Title: Phase I/II Trial of H3B-6545, a Novel Selective Estrogen Receptor Covalent Antagonist (SERCA), in Estrogen Receptor Positive (ER+), Human Epidermal Growth Factor Receptor 2 Negative (HER2-) Advanced Breast Cancer
Session: PD8-06
Date and Time: Thursday, December 10, 2020, 2:15pm – 3:30pm CT
Presenter: Erika P. Hamilton, Sarah Cannon Research Institute, Tennessee Oncology

Abstract Number: 1268
Title: Pharmacokinetics of H3B-6545 in Patients with Locally Advanced or Metastatic Estrogen Receptor-Positive HER2 Negative Breast Cancer (ER+ and HER2- BC)
Session: PS12-15
Date and Time: Wednesday, December 9, 2020, 8:00am CT
Presenter: Oneeb Majid, Eisai Ltd.

Abstract Number: 918
Title: Development of H3B-6545, a First-in-Class Oral Selective ER Covalent Antagonist (SERCA), for the Treatment of ERWT and ERMUT Breast Cancer
Session: PS12-23
Date and Time: Wednesday, December 9, 2020, 8:00am CT
Presenter: Manav Korpal, H3 Biomedicine, Inc.

About H3B-6545
Estrogen receptor alpha (ERα) plays an important oncogenic role in the genesis and progression of luminal breast cancers and historically has been a target of endocrine therapies. However, recently, hotspot mutations in ERα have been detected in nearly 30% of endocrine-therapy resistant metastases. Functional studies have shown that these ERα mutations can confer ligand-independent activation of the ERα pathway and can promote partial resistance to existing classes of ER-directed therapies. H3B-6545, a first-in-class small molecule selective estrogen receptor covalent antagonist (SERCA) demonstrates activity in tumor models that harbor wild-type or mutant ERα. H3B-6545 activity against ERα mutants resistant to standard therapy provides an opportunity to target a currently unmet medical need both as a single agent and in combination with other breast cancer therapies.

This release discusses investigational uses of agents in development and is not intended to convey conclusions about efficacy or safety. There is no guarantee that such investigational agents will successfully complete clinical development or gain health authority approval.

Curis Announces Positive Preliminary Data from Ongoing Phase 1 Study of CA-4948 Monotherapy in Patients with Relapsed or Refractory Acute Myeloid Leukemia and Myelodysplastic Syndromes

On December 8, 2020 Curis, Inc. (NASDAQ: CRIS), a biotechnology company focused on the development of innovative therapeutics for the treatment of cancer, reported positive preliminary data from its ongoing open-label, single arm Phase 1 dose escalation study of CA-4948, a novel, small molecule IRAK4 kinase inhibitor, in patients with acute myeloid leukemia (AML) or high-risk myelodysplastic syndromes (MDS) (Press release, Curis, DEC 8, 2020, View Source [SID1234572401]). IRAK4 plays an essential role in the toll-like receptor (TLR) and interleukin-1 receptor (IL-1R) signaling pathways, and these pathways are frequently dysregulated in patients with AML and MDS. Third parties have recently discovered that the long form of IRAK4 (IRAK4-L) is oncogenic and preferentially expressed in over half of patients with AML and MDS. A variety of drivers are believed to cause this, including specific spliceosome mutations.

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"We are highly encouraged by the breadth of clinical activity with CA-4948 seen with this early data, especially as this study is both monotherapy and in a late line, relapsed/refractory population. Historically, monotherapy studies in AML and MDS have proven underwhelming; monotherapy studies in a relapsed/refractory setting have been especially challenging," said James Dentzer, President and Chief Executive Officer of Curis. "We also have been pleased by the pace at which our trial partners have been able to enroll patients. We look forward to continuing to advance CA-4948 and reporting additional Phase 1 data in the second half of 2021."

"As a clinician intimately familiar with the treatment challenges faced by patients with AML or high-risk MDS, I am very encouraged by the early data coming out of this study," said Dr. Guillermo Garcia-Manero, Chief of the Section of Myelodysplastic Syndromes within the Department of Leukemia at The University of Texas MD Anderson Cancer Center. "While there have been important advancements in the development of new therapeutics for patients with previously untreated AML or MDS in recent years, relapsed and refractory patients are still in need of better treatment options. These preliminary data suggest, for the first time in a clinical setting, that successfully targeting the long isoform of IRAK4, which we know to be preferentially expressed in over half of AML and MDS patients, could be the first major breakthrough in over a decade for patients with these diseases."

The reported preliminary data are from Curis’s ongoing open-label, single arm Phase 1 dose escalation 3+3 study of orally administered CA-4948 monotherapy in adult patients with AML or high-risk MDS. A minimum of 3 patients will be enrolled in each cohort of the two-part study, starting with 200 mg BID, which was demonstrated to be well-tolerated, capable of achieving relevant levels of drug exposure and has demonstrated signs of biologic activity in Curis’s ongoing Phase 1 study of CA-4948 for the treatment of patients with relapsed or refractory non-Hodgkin’s lymphoma. The primary objective of the study is to determine the maximum tolerated dose (MTD) and recommended Phase 2 dose (RP2D) for CA-4948 based on safety and tolerability, dose-limiting toxicities (DLT), and any biologic activity, pharmacokinetic and pharmacodynamic findings from the study trial population. Additional objectives include characterization of CA-4948’s pharmacokinetic parameters, and biomarker correlations. As of November 23, 2020, 4 AML patients and 3 high-risk MDS patients had been enrolled in the first 2 study cohorts and no DLTs had been observed. The data being reported from this ongoing trial are preliminary and subject to change.

Key findings include:

Marrow blast reductions observed in all evaluable patients (6 patients).
6 of 7 patients enrolled remain on study.
Patients enrolled experienced a median of 3 prior lines of treatment (range 1-4).
Two patients experienced a marrow complete response, one with blast count going from 23% pretreatment to 1% on treatment, and the other going from 11% pretreatment to 2% on treatment.
No DLTs observed in 7 DLT-evaluable patients in the 200 mg BID and 300 mg BID cohorts.
Enrollment has begun in the 400 mg BID cohort.
Webcast Event Information

Curis management will host a virtual KOL event today, December 8, 2020 at 8:00 am ET to discuss these results with Dr. Amit Verma, Professor of Medicine-Oncology at Albert Einstein College of Medicine, and Director of the MDS Program at Montefiore Medical Center located in Bronx, NY. To access the webcast, please visit the Events and Presentations section of the Curis website at View Source