Monopar Announces Initiation of its Phase 2b/3 (VOICE) Trial to Evaluate Validive® for the Prevention of Chemoradiotherapy-Induced Severe Oral Mucositis (SOM) in Oropharyngeal Cancer (OPC)

On December 8, 2020 Monopar Therapeutics Inc. (Nasdaq: MNPR), a clinical-stage biopharmaceutical company primarily focused on developing proprietary therapeutics designed to extend life or improve the quality of life for cancer patients, reported that its Phase 2b/3 clinical trial of Validive for the prevention of chemoradiotherapy-induced severe oral mucositis in patients with oropharyngeal cancer (VOICE) is active and recruiting patients (Press release, Monopar Therapeutics, DEC 8, 2020, View Source [SID1234572428]).

"We are pleased to have multiple clinical sites activated," said Andrew Mazar, PhD, Chief Scientific Officer of Monopar, "and are looking forward to dosing the first patients shortly."

"The commencement of our Phase 2b/3 VOICE trial is a significant milestone for Monopar and, it represents a key step in the development of a therapy that could benefit many OPC patients," said Chandler Robinson, MD, Chief Executive Officer of Monopar. "This trial builds on the foundation of the completed Phase 2, and is designed to confirm Validive reduces the incidence of SOM in OPC patients undergoing chemoradiotherapy." The completed Phase 2 trial showed the incidence of SOM in OPC patients receiving Validive 100 µg to be 40% lower compared to those receiving placebo.

It is estimated there will be greater than 40,000 new OPC patients in the U.S. alone in 2021, the majority of whom will be treated with chemoradiation and run substantial risk of developing SOM. Currently, there is no FDA approved preventive or treatment for SOM in these patients, emphasizing the clear unmet medical need in this patient population.

Up to approximately 260 patients will be enrolled in this multi-center, randomized, double-blind, placebo-controlled, Phase 2b/3 clinical trial. The trial includes an interim analysis, which is anticipated to be reached approximately twelve months after the first patient is dosed.

Further information about the Validive Phase 2b/3 VOICE trial is available at www.ClinicalTrials.gov under study identifier NCT 04648020.

About Validive
Validive (clonidine mucobuccal tablet; clonidine MBT) is a novel mucobuccal tablet (MBT) formulation of clonidine which provides for prolonged and enhanced local delivery of clonidine to the regions of mucosal radiation damage in OPC patients. The tablet is self-administered once daily in the patient’s home setting with the patient placing it under the upper lip where it adheres to the gums and dissolves over several hours, continuously releasing the clonidine into the saliva. Clonidine agonizes the alpha-2 adrenergic receptor on macrophages (white blood cells present in the immune tissues of the oropharynx), decreasing the macrophages’ expression of destructive cytokines they tend to release in response to radiotherapy. A completed double-blind, randomized, placebo-controlled Phase 2 clinical trial of Validive showed reduced incidence (absolute decrease of 26%, relative decrease of 40%) in OPC patients treated with Validive 100 µg (a meaningful trend in the Phase 2, which the Phase 2b/3 is designed to confirm with a larger trial in OPC for potential statistical significance), a safety profile similar to the placebo, and a high rate of treatment compliance (over 90%).

About Severe Oral Mucositis
Severe oral mucositis (SOM) is a painful and debilitating inflammation and ulceration of the mucous membranes lining the oral cavity and oropharynx in response to insult such as chemoradiation treatment (CRT). SOM is the most frequent major side effect experienced by oropharyngeal cancer patients, experienced by a majority of those undergoing CRT. SOM impacts both quality of life and clinical outcomes for these patients. SOM prevents patients from drinking and/or eating, and can lead to severe weight loss, opiate usage, and the use of feeding tubes as well as intravenous supplementation to keep alive. Patients who develop SOM can become hospitalized, and symptoms can force patients to prematurely stop cancer treatment, reducing treatment efficacy and long-term survival.

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Regulus Therapeutics Announces Closing of $19.4 Million Private Placement of Equity

On December 8, 2020 Regulus Therapeutics Inc. (Nasdaq: RGLS), a biopharmaceutical company focused on the discovery and development of innovative medicines targeting microRNAs, reported the closing of its previously announced private placement of equity (Press release, Regulus, DEC 8, 2020, View Source [SID1234572427]). The Company received gross proceeds of approximately $19.4 million from the sale of 24,341,607 shares of the Company’s common stock ("Common Stock") and accompanying warrants to purchase up to an aggregate of 18,256,204 shares of Common Stock at a purchase price of $0.622 per share of Common Stock and $0.125 for each share of Common Stock underlying such warrants. In addition, the Company sold 272,970 shares of non-voting Class A-3 convertible preferred stock, in lieu of shares of Common Stock, at a price of $6.22 per share, and accompanying warrants to purchase an aggregate of 2,047,276 shares of Common Stock at a price of $0.125 for each share of Common Stock underlying these warrants. Each share of non-voting Class A-3 convertible preferred stock is convertible into 10 shares of Common Stock, subject to certain beneficial ownership conversion limitations. The Company expects to use the net proceeds from the transaction primarily to advance RGLS4326 for the treatment of Autosomal Dominant Polycystic Kidney Disease and for general corporate purposes. H.C. Wainwright and Co. acted as exclusive placement agent for the financing.

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The offer and sale of the foregoing securities were made in a transaction not involving a public offering and have not been registered under the Securities Act of 1933, as amended (the "Securities Act"), or applicable state securities laws. Accordingly, the securities may not be reoffered or resold in the United States except pursuant to an effective registration statement or an applicable exemption from the registration requirements of the Securities Act and such applicable state securities laws.

This press release does not constitute an offer to sell or the solicitation of an offer to buy the securities, nor shall there be any sale of the securities in any state in which such offer, solicitation or sale would be unlawful prior to the registration or qualification under the securities laws of such state.

Additional details regarding the private placement are included in the Form 8-K filed with the Securities and Exchange Commission on December 4, 2020.

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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