CT 1812

New Drug Approvals

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CT-1812

Elayta

Condition(s): Alzheimer’s Disease
U.S. FDA Status: Alzheimer’s Disease (Phase 2)
Company: Cognition Therapeutics Inc.

CAS: 1802632-22-9
Chemical Formula: C24H33NO4S
Molecular Weight: 431.591

2-(tert-butoxy)-4-(3-methyl-3-(5-(methylsulfonyl)isoindolin-2-yl)butyl)phenol

Phenol, 4-[3-[1,3-dihydro-5-(methylsulfonyl)-2H-isoindol-2-yl]-3-methylbutyl]-2-(1,1-dimethylethoxy)-

  • Originator Cognition Therapeutics
  • Class Antidementias; Neuroprotectants; Nootropics; Small molecules
  • Mechanism of Action Sigma-2 receptor antagonists
  • Phase II Alzheimer’s disease
  • Phase I Cognition disorders
  • 21 Feb 2019 Cognition Therapeutics receives patent for a composition of matter patent covering Elayta™ in Europe
  • 19 Feb 2019 Pharmacokinetics and adverse events data from a phase I trial in Cognition disorders released by Cognition Therapeutics
  • 22 Oct 2018 CTP push 289675: Updated KDM, forwarded USA line from PI/II to PII

CT-1812 is a first-in-class, orally available sigma-2/PGRMC1 antagonist (alpha beta oligomer receptor antagonist), is being developed by Cognition. sCT-1812 is a novel therapeutic candidate for Alzheimer’s disease

SYN

BACKGROUND

CT1812 is a small-molecule antagonist of the sigma2 receptor, also known as the progesterone receptor membrane component 1…

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ACLIMOSTAT

New Drug Approvals

imgImage result for Aclimostat

Aclimostat
CAS: 2082752-83-6
Chemical Formula: C26H42N2O6
Molecular Weight: 478.63
Elemental Analysis: C, 65.25; H, 8.85; N, 5.85; O, 20.06

ZGN-1061; ZGN1061; ZGN 1061; Aclimostat,

UNII-X150A3JK8R

X150A3JK8R

(3R,4S,5S,6R)-5-Methoxy-4-[(2R,3R)-2-methyl-3-(3- methylbut-2-en-1-yl)oxiran-2-yl]-1-oxaspiro[2.5]octan-6-yl 3-[2-(morpholin-4-yl)ethyl]azetidine-1-carboxylate

1-Azetidinecarboxylic acid, 3-[2-(4-morpholinyl)ethyl]-, (3R,4S,5S,6R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-methyl-2-buten-1-yl)-2-oxiranyl]-1-oxaspiro[2.5]oct-6-yl ester

3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1- oxaspiro[2.5]octan-6-yl 3-(2-morpholinoethyl)azetidine-1-carboxylate

ZAFGEN,  PHASE 2,  DIABETES

Aclimostat, also known as ZGN-1061, is an anti-diabetic, anti-obesity MetAP2 inhibitor.

Over 1.1 billion people worldwide are reported to be overweight. Obesity is estimated to affect over 90 million people in the United States alone. Twenty-five percent of the population in the United States over the age of twenty is considered clinically obese. While being overweight or obese presents problems (for example restriction of mobility, discomfort in tight spaces such as theater or airplane seats, social difficulties, etc.), these conditions, in particular clinical obesity, affect other aspects of health, i.e., diseases and other adverse health conditions associated…

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Peficitinib hydrobromide, ペフィシチニブ臭化水素酸塩

New Drug Approvals

1353219-05-2.pngStructure of PEFICITINIB HYDROBROMIDEimgChemSpider 2D Image | PEFICITINIB HYDROBROMIDE | C18H23BrN4O2

Peficitinib hydrobromide

ペフィシチニブ臭化水素酸塩

ASP015K,

Rheumatoid Arthritis

1H-Pyrrolo(2,3-b)pyridine-5-carboxamide, 4-((5-hydroxytricyclo(3.3.1.13,7)dec-2-yl)amino)-, hydrobromide (1:1), stereoisomer

4-{[(1R,2s,3S,5r)-5-Hydroxyadamantan-2-yl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrobromide (1:1)

1H-Pyrrolo[2,3-b]pyridine-5-carboxamide, 4-[[(1R,3S)-5-hydroxytricyclo[3.3.1.13,7]dec-2-yl]amino]-, hydrobromide (1:1)

U55XHZ5X6P

Formula
C18H22N4O2. HBr
CAS
1353219-05-2 HBR
944118-01-8 BASE
Mol weight
407.3048

PMDA, 2019/3/26 JAPAN APPROVED, Smyraf

Image result for Peficitinib hydrobromide

Peficitinib hydrobromide is used in the treatment of Psoriasis and Rheumatoid Arthritis

Peficitinib (formerly known as ASP015K) is a pyrrolo[2,3-b]pyridine derivative orally administered once-daily JAK inhibitor in development for the treatment of Rheumatoid Arthritis. In preclinical studied Peficitinib inhibited JAK1 and JAK3 with IC50 of 3.9 and 0.7 nM, respectively. Peficitinib also inhibited IL-2-dependent T cell proliferation in vitro and STAT5 phosphorylation in vitro and ex vivo. Furthermore, Peficitinib dose-dependently suppressed bone destruction and paw swelling in an adjuvant-induced arthritis model in rats via prophylactic or therapeutic oral dosing regimens.In clinical trials, Peficitinib treatment prescribed at 50, 100 and 150 mg amounts each showed statistically significantly higher ACR20 response rates compared to the placebo and response…

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VNRX-7145

New Drug Approvals

str1

str1

CAS 1842399-68-1

MF C19 H26 B N O7

MW 391.22

2H-1,2-Benzoxaborin-8-carboxylic acid, 3,4-dihydro-2-hydroxy-3-[(1-oxopropyl)amino]-, (2-ethyl-1-oxobutoxy)methyl ester, (3R)-

The VNRX-7145 combination is now in Phase I studies to treat resistant urinary tract infections.

str1

VNRX-7145

PATENT

WO 2015191907

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2015191907

ntibiotics are the most effective drugs for curing bacteria-infectious diseases clinically. They have a wide market due to their advantages of good antibacterial effect with limited side effects. Among them, the beta-lactam class of antibiotics (for example, penicillins, cephalosporins, and carbapenems) is widely used because they have a strong bactericidal effect and low toxicity.

[0005] To counter the efficacy of the various beta-lactams, bacteria have evolved to produce variants of beta-lactam deactivating enzymes called beta-lactamases, and in the ability to share this tool inter- and intra-species. These beta-lactamases are categorized as“serine” or“metallo” based, respectively, on presence of a key serine or zinc in the enzyme active site. The rapid…

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Prabotulinumtoxin A, プラボツリナムトキシンA

New Drug Approvals

>Botulinum Toxin Type A Sequence
MPFVNKQFNYKDPVNGVDIAYIKIPNVGQMQPVKAFKIHNKIWVIPERDTFTNPEEGDLN
PPPEAKQVPVSYYDSTYLSTDNEKDNYLKGVTKLFERIYSTDLGRMLLTSIVRGIPFWGG
STIDTELKVIDTNCINVIQPDGSYRSEELNLVIIGPSADIIQFECKSFGHEVLNLTRNGY
GSTQYIRFSPDFTFGFEESLEVDTNPLLGAGKFATDPAVTLAHELIHAGHRLYGIAINPN
RVFKVNTNAYYEMSGLEVSFEELRTFGGHDAKFIDSLQENEFRLYYYNKFKDIASTLNKA
KSIVGTTASLQYMKNVFKEKYLLSEDTSGKFSVDKLKFDKLYKMLTEIYTEDNFVKFFKV
LNRKTYLNFDKAVFKINIVPKVNYTIYDGFNLRNTNLAANFNGQNTEINNMNFTKLKNFT
GLFEFYKLLCVRGIITSKTKSLDKGYNKALNDLCIKVNNWDLFFSPSEDNFTNDLNKGEE
ITSDTNIEAAEENISLDLIQQYYLTFNFDNEPENISIENLSSDIIGQLELMPNIERFPNG
KKYELDKYTMFHYLRAQEFEHGKSRIALTNSVNEALLNPSRVYTFFSSDYVKKVNKATEA
AMFLGWVEQLVYDFTDETSEVSTTDKIADITIIIPYIGPALNIGNMLYKDDFVGALIFSG
AVILLEFIPEIAIPVLGTFALVSYIANKVLTVQTIDNALSKRNEKWDEVYKYIVTNWLAK
VNTQIDLIRKKMKEALENQAEATKAIINYQYNQYTEEEKNNINFNIDDLSSKLNESINKA
MININKFLNQCSVSYLMNSMIPYGVKRLEDFDASLKDALLKYIYDNRGTLIGQVDRLKDK
VNNTLSTDIPFQLSKYVDNQRLLSTFTEYIKNIINTSILNLRYESNHLIDLSRYASKINI
GSKVNFDPIDKNQIQLFNLESSKIEVILKNAIVYNSMYENFSTSFWIRIPKYFNSISLNN
EYTIINCMENNSGWKVSLNYGEIIWTLQDTQEIKQRVVFKYSQMINISDYINRWIFVTIT
NNRLNNSKIYINGRLIDQKPISNLGNIHASNNIMFKLDGCRDTHRYIWIKYFNLFDKELN
EKEIKDLYDNQSNSGILKDFWGDYLQYDKPYYMLNLYDPNKYVDVNNVGIRGYMYLKGPR
GSVMTTNIYLNSSLYRGTKFIIKKYASGNKDNIVRNNDRVYINVVVKNKEYRLATNASQA
GVEKILSALEIPDVGNLSQVVVMKSKNDQGITNKCKMNLQDNNGNDIGFIGFHQFNNIAK
LVASNWYNRQIERSSRTLGCSWEFIPVDDGWGERPL

Prabotulinumtoxin A

プラボツリナムトキシンA;

Db00083

Formula
C6760H10447N1743O2010S32
CAS
93384-43-1
Mol weight
149320.8333

AGN 191622 / ANT-1207 / ANT-1401 / ANT-1403 / NT 201

        • APPROVED , FDA 2019, Jeuveau, 2019/2/1

Image result for Prabotulinumtoxina

  • Purified botulinum toxin from Clostridium botulinum, purified from culture via dialysis and acid precipitation.
  • Originator Daewoong Pharmaceutical
  • Developer Daewoong Pharmaceutical; Evolus
  • Class Analgesics; Antidepressants; Antimigraines; Antispasmodics; Bacterial proteins; Bacterial toxins; Botulinum toxins; Eye disorder therapies; Muscle relaxants; Skin disorder therapies; Urologics
  • Mechanism of Action Acetylcholine inhibitors; Glutamate antagonists; Membrane transport protein modulators; Neuromuscular blocking agents
  • Marketed Glabellar lines
  • Phase III Muscle spasticity
  • Phase II/III Blepharospasm; Facial wrinkles
  • 27 Feb 2019 Evolus plans to launch prabotulinumtoxin A for Glabellar lines in USA (IM)
  • 01 Feb 2019 Registered for Glabellar lines in USA (IM)
  • 26 Nov 2018 Daewoong Pharmaceutical expects…

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FDA permits marketing of two devices that detect parathyroid tissue in real-time during surgery

FDA permits marketing of two devices that detect parathyroid tissue in real-time during surgery
Today, the U.S. Food and Drug Administration permitted marketing of two devices that provide real-time location of parathyroid tissue during surgical procedures such as thyroidectomy (surgery to remove all or part of the thyroid) and parathyroidectomy (surgery to remove one or more parathyroid glands).
“For some patients with parathyroid disease, treatment may mean a surgical procedure,” said Binita Ashar, M.D., director of the Division of Surgical Devices in the FDA’s Center for Devices and Radiological Health.  “Real-time identification of parathyroid tissue during surgery can provide surgeons… Continue reading.

https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm624982.htm?utm_campaign=11022018_PR_FDA%20authorizes%20devices%20to%20detect%20parathyroid%20tissue%20in%20during%20surgery&utm_medium=email&utm_source=Eloqua

November 2, 2018

Release

Today, the U.S. Food and Drug Administration permitted marketing of two devices that provide real-time location of parathyroid tissue during surgical procedures such as thyroidectomy (surgery to remove all or part of the thyroid) and parathyroidectomy (surgery to remove one or more parathyroid glands).

“For some patients with parathyroid disease, treatment may mean a surgical procedure,” said Binita Ashar, M.D., director of the Division of Surgical Devices in the FDA’s Center for Devices and Radiological Health. “Real-time identification of parathyroid tissue during surgery can provide surgeons with valuable information to help preserve healthy tissue or to remove diseased tissue.”

Disorders in the parathyroid tissue, which is tissue that borders the thyroid gland, are usually treated by surgeries to remove part of the thyroid gland or parathyroid tissue. Hyperparathyroidism, or the overproduction of parathyroid hormone, is the most common of parathyroid disorders and is diagnosed in approximately 100,000 Americans each year. For surgeons treating hyperparathyroidism or other disorders, parathyroid tissue can be visually difficult to locate and distinguish from nearby tissues during a surgery.

The Fluobeam 800 Clinic Imaging Device is used to assist in the imaging of parathyroid glands and can be used as a companion method to assist surgeons in locating parathyroid tissue visually during surgery. Parathyroid tissue emits a fluorescent glow when exposed to the device’s light source, avoiding the need for a contrast agent. The device was previously cleared as an imaging system used to capture and view fluorescent images for the visual assessment of blood flow as an adjunctive method for the evaluation of tissue perfusion.

The Parathyroid Detection PTeye System aids in detecting parathyroid tissue during surgery by using a probe that emits fluorescence light. Tissue detection is based on how the parathyroid tissue reacts to the fluorescent light. When parathyroid tissue is detected, the system provides an audio and visual display to indicate its presence.

Use of either device is intended to assist, not replace, experienced visual assessment in identifying the parathyroid tissue along with a biopsy to confirm thyroid tissue per standard of care. The systems are not intended to be used to confirm the absence of parathyroid tissue or glands and are only to be used to assist the surgeon in locating potential parathyroid tissue or glands.

For the Fluobeam 800, the FDA reviewed data from five peer-reviewed published studies, including one study that compared the rate of postoperative hypocalcemia (PH), or a temporary reduction in calcium in the blood, that occurs when healthy parathyroid tissue is inadvertently removed. In 93 patients who had surgery using the device, 5 percent experienced fluctuating PH following surgery compared with 21 percent of the 153 patients who had surgery without the device.

For the PTeye System, the FDA reviewed data from a single-blinded study of 81 patients who had surgery using the device. Results demonstrated that the PTeye could correctly identify the presence of parathyroid tissue as compared to histology 93 percent of the time and correctly identify the absence of parathyroid tissue as compared to intraoperative visualization by an expert 97 percent of the time, with an overall accuracy of 96 percent.

The Fluobeam 800 and the PTeye were reviewed separately but concurrently under the FDA’s De Novo premarket review pathway, a regulatory pathway for some low- to moderate-risk devices that are novel and for which there is no prior legally marketed device.

The FDA granted marketing authorization of The Fluobeam 800 Clinic Imaging Device to Fluoptics.

The FDA granted marketing authorization of Parathyroid Detection PTeye System to AiBiomed.

///////////////FDA, marketing, devices, parathyroid tissue, surgery, marketing authorization, Parathyroid Detection PTeye System, AiBiomed.

Statement from FDA Commissioner Scott Gottlieb, M.D., on findings from the romaine lettuce E. coli O157:H7 outbreak investigation and FDA’s efforts to prevent future outbreaks

tatement from FDA Commissioner Scott Gottlieb, M.D., on findings from the romaine lettuce E. coli O157:H7 outbreak investigation and FDA’s efforts to prevent future outbreaks

Earlier this year, we experienced the largest E. coli O157:H7 outbreak the country has seen in the last decade, leaving hundreds sick and claiming the lives of five people who consumed contaminated romaine lettuce.
We’re committed to taking necessary actions to prevent future outbreaks like this and to improving the safety of leafy greens available in the marketplace. Since the next romaine growing season for the Yuma region is underway, it’s critical for all of us to understand what happened so we can identify the changes that can prevent future outbreaks and reduce the scope of any problems that could arise.
Since the first signs of the outbreak appeared…Continue reading

https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm624867.htm?utm_campaign=11012018_Statement_findings%20from%20the%20romaine%20lettuce%20E.%20coli%20O157%3AH7&utm_medium=email&utm_source=Eloqua

November 1, 2018

Statement

Earlier this year, we experienced the largest E. coli O157:H7 outbreak the country has seen in the last decade, leaving hundreds sick and claiming the lives of five people who consumed contaminated romaine lettuce.

We’re committed to taking necessary actions to prevent future outbreaks like this and to improving the safety of leafy greens available in the marketplace. Since the next romaine growing season for the Yuma region is underway, it’s critical for all of us to understand what happened so we can identify the changes that can prevent future outbreaks and reduce the scope of any problems that could arise.

Since the first signs of the outbreak appeared, our team has collaborated closely with our state, federal and local partners to determine the root cause of the outbreak. Today, the U.S. Food and Drug Administration is sharing an environmental assessment that details final findings from this investigation.

One of the investigation’s main objectives was to identify factors that potentially contributed to the introduction and spread of the strain of E. coli O157:H7 that contaminated the romaine lettuce associated with this outbreak. The FDA, the Centers for Disease Control and Prevention, and the Arizona Department of Agriculture launched an investigation of the outbreak, leading to the collection of samples in Yuma in order to help gather evidence needed to identify the source of the outbreak.

The environmental assessment issued today confirms the presence of E. coliO157:H7 in three samples of irrigation canal water collected as part of this investigation in the Yuma region. It considers that the most likely way the romaine lettuce became contaminated was from the use of water from the irrigation canal, since the outbreak strain was not found in any of the other samples collected in the region. How the water contaminated the lettuce is uncertain. But based on interviews with growers and pesticide applicators, possible explanations include direct application of irrigation canal water to the lettuce crop or the use of irrigation canal water to dilute crop-protection chemicals applied to the crops through both aerial and land-based spray applications. We cannot rule out other ways the lettuce became contaminated. It’s important to note that we have no evidence that any other product grown in Yuma was contaminated by this water.

When and how the irrigation canal became contaminated with the outbreak strain of E. coli O157:H7 is also uncertain. We know that a large concentrated animal feeding operation (CAFO) is located adjacent to this stretch of the irrigation canal where the samples were collected. This is one potential source. However, the investigation did not identify an obvious route for contamination of the irrigation canal from this facility. In addition, samples collected at the CAFO did not yield E. coli O157:H7. The investigation did not exclude other ways the irrigation canal could have become contaminated with this outbreak strain.

With the growing season underway in Yuma, we know just how important it is to continue collaborating closely with industry and our regulatory partners to ensure that leafy greens are safe. To assist with these efforts, our environmental assessment recommends a number of steps that can be taken to reduce the likelihood of another tragic outbreak from occurring in the future. Working with the produce industry to further reduce the risk of outbreaks is a key priority for the FDA.

Fully implementing the Food Safety Modernization Act (FSMA) is critical to these efforts. We must continue to advance FSMA’s Produce Safety Rule in collaboration with our state regulatory partners and ensure that we craft agricultural water standards that work across the incredible diversity of commodities and growing conditions. The FDA has resources available to help industry comply with FSMA requirements, including produce safety experts regionally located as part of the FDA’s Produce Safety Network and growers in the Yuma region can find the contact information for their area at this website.

Because leafy greens are a highly perishable commodity, the ability to traceback the route of a food product as it moves through the entire supply chain, or traceability, is critical to removing the product from commerce as quickly as possible, preventing additional consumer exposures, and properly focusing any recall actions. During the romaine investigation we found the typical traceback process to be particularly challenging because much of the finished lettuce product contained romaine that was sourced from multiple ranches As a result, our investigation involved collecting documentation from each point in the supply chain to verify the movement of product back to the Yuma area. Complicating this already large-scale investigation, the majority of the records collected in this investigation were either paper or handwritten.

Going forward, both FDA and industry need to explore better ways to standardize record keeping and determine whether the use of additional tools on product packaging could improve traceability.

We strongly encourage the leafy greens industry to adopt traceability best practices and state-of-the-art technologies to help assure quick and easy access to key data elements from farm to fork. We also strongly encourage the leafy greens industry to explore modern approaches to standardized record keeping and the use of additional tools or labels on product packaging that could improve traceability. We urge all segments of this industry and our government partners to review the findings of our environmental assessment and make necessary changes. For our part, the FDA is exploring ways to best tap into new technologies to significantly reduce the time needed for traceback investigations.

The agency is taking steps to improve our response times and provide actionable information to consumers as quickly as possible. We are also looking at our regulatory options and considering appropriate enforcement actions against companies and farms that grow, pack, or process fresh lettuce and leafy greens under insanitary conditions. We continue to explore additional ways to improve these processes and urge all segments of the leafy greens industry to review their operations in the same way.

As a next step, the FDA plans to collect and analyze romaine lettuce samples through a new special surveillance sampling assignment for contamination with human pathogens. This will help us determine whether products are safe to enter the U.S. marketplace. If samples are found to be contaminated, the FDA will follow-up with fresh-cut leafy greens processors and their growers or suppliers to determine if these foods were produced under insanitary conditions that render them harmful to consumers and take the appropriate action to remove them from the market.

We recognize and appreciate the efforts that the leafy greens industry has taken to date. But we know more must be done on all fronts to help prevent future foodborne illness outbreaks. I remain committed to investing in the FDA’s food program and applying our food safety expertise as we work to better safeguard the U.S. food supply. We want food to be safe because it promotes the American industries that grow and produce these products. That’s part of our dedication to these efforts. But first and foremost, we pursue food safety measures as key parts of our public health mandate to protect American consumers

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