API and IP Newsletter

Contents 

• Bromo derivatives used in early stage of development 

• General information. 

• Biophore applies to DCGI for emergency-use approval for COVID-19 treatment drug.

• China on the Move: An Improving Regulatory Landscape with New Challenges Ahead –Genomics and National Security. 

• Intellectual Property. 

• Claim construction decision by NJ Court about Levomilnacipram.. 

Bromo derivatives used in early stage of development

In our firm we analyse import/ export database. We analysed several types of compounds, usually required in API manufacturing. We study import databases to understand development progress of many Indian Gx companies.

In our assessment, bromination and manufacturing of bromo derivatives would always be a challenge for Indian manufacturers. The most of bromo derivatives are being imported from China.

We listed several bromo derivatives which are being imported by Indian companies for their APIs which are under development. In this news article, we are providing glimpses of data collected about bromo derivatives, bromination and our analysis. 

Intermediate	API	Importer	FDA approval	SIDVIM comments
(3R 4S)-3-(2-BROMOACETYL)-4-ETHYL-1-PYRROLIDINECARBOXYLIC ACID PHENYLMETHYL ESTER	Upadacitinib	DRL	Aug-19	DRL and Aurobindo should be filing DMF for Upadacitinib soon?
		Aurobindo
(4AS 9BR)-ETHYL 6-BROMO-5-(2-(METHYLAMINO)-2-OXOETHYL)-3 4 4A 5-TETRAHYDRO-1H-PYRIDO[4 3-B]INDOLE-2(9BH)-CARBOXYLATE	Lumateperone	DRL	Dec-19	DRL, Alembic and Aurigene are active in API synthesis.
		Alembic
		Aurigene
1-BROMO-2-CHLOROBENZENE	Ketamine	Aap Pharma	Old approval	Few active ANDAs but there is one DMF so far. Only 2 main exporters of APIs. Smart product selection by Aap?
1-BROMO-3 5-DIMETHYL ADAMANTANE	Memantine	Aurobindo	Dec-14	Two DMFs filed. Couple of ANDA approved. Aurobindo had also approved ANDA. Aurobindo must be trying to produce own API and file DMF.
1-BROMO-3-METHOXYPROPANE	Brinzolamide	Alembic	Apr-13	No DMF filed yet. Alembic must be in process of filing DMF.
2 3-DIBROMO-5-CHLORO-PYRIDINE	Ubrogepant	DRL	Dec-19	At least three companies (DRL, Aurobindo and Cipla) are working on Gx versions of Ubrogepant
		Aurobindo
		Cipla
2-BROMO-5-FLUORO-4-NITROANILINE	Tezacaftor	Aurobindo	Feb-18	Combi product approved in 2018
		Hetero

General information

Biophore applies to DCGI for emergency-use approval for COVID-19 treatment drug

Aviptadil is a synthetic form of Vasoactive Intestinal Peptide. Drugmaker Biophore India Pharmaceuticals on Friday said it has applied to the Drugs Controller General of India (DCGI) seeking emergency use approval for Aviptadil Inhalation in the treatment of moderate to severe COVID-19. (Read more)

China on the Move: An Improving Regulatory Landscape with New Challenges Ahead –Genomics and National Security

In the past, the Center for Drug Evaluation (CDE) took about 900 days to review and approve a drug registration. This procedure was shortened to about 300 days in 2019. A direct reason for the reduction is that CDE staff increased from 100 in 2015 to about 1000 in 2020.

Similar to the U.S. Food and Drug Administration (FDA), China’s National Medical Products Administration (NMPA) established certain fast tracks for the registration of drugs with significant therapeutic value: priority review and approval, breakthrough therapy designation (BTD), and conditional approval. Innovative drugs with significant clinical value may apply for the fast tracks. The time for priority review and approval may be further shortened to 130 working days or even 70 working days, if the drug has been marketed overseas. (Read more)

Intellectual Property

Claim construction decision by NJ Court about  Levomilnacipram

Levomilnacipran is used to treat depression. It works by increasing the amount of serotonin and norepinephrine, natural substances in the brain that helps maintain mental balance.

As per available information, in the last quarter ER capsules sales was about $ 117 mio (Read more)

Below are the patents listed in OB.

Patent No	Patent Expiration	Drug Substance	Drug Product	Patent Use Code	Submission Date
8481598	03/02/2031			U-839	08/15/2013
8865937	05/23/2032	DS	DP		11/20/2014
RE43879	01/11/2026			U-839	08/15/2013

Hikma, Amneal Gx version is approved. But Gx version is not available in market as per public domain information.

Claim granted US 8,481,598 B2 issued to Forest (Allergan) as follows 

1.     A method for treating major depressive disorder in a patient in need thereof, comprising administering to the patient about 120 mg/day of Levomilnacipran or a pharmaceutically acceptable salt-------

Aurobindo, MSN, Torrent and Zydus filed PIV and argued claim is stating Levomilnacipran 120 mg/day or Levomilnacipram salt 120 mg/day.

Patentee disagreed, claimed it should be construed as 120 mg/day or molecular weight equivalent of the salt of Levomilnacipram.

Court agreed with the patentee.

More details here.

Disclaimer

Sidvim LifeSciences Private Ltd has taken due care and caution in developing this document. Since the data used for analysis in this document is based on the information available in the public domain, its adequacy or accuracy or completeness cannot be guaranteed. This document is for information only and Sidvim is not responsible for losses that may or may not arise due to any decisions made based on the same. No part of the document shall constitute or be represented as a legal opinion of any kind or nature. No warranties or guarantees, expressed or implied, are included in or intended by the document, except that it has been prepared in accordance with the current generally accepted practices and standards consistent with the level of care and skill exercised under similar circumstances by professional consultants or firms that perform the same or similar services.