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Synopsis

Synopsis

ACTIVE PHARMA INGREDIENTS

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USDMF

US DMFs Filed

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CEP/COS

CEP/COS Certifications

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JDMF

JDMFs Filed

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EU WC

EU WC

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KDMF

KDMF

API REF. PRICE (USD/KG)

MARKET PLACE

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FDF

FINISHED DOSAGE FORMULATIONS

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Europe

Europe

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Australia

Australia

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South Africa

South Africa

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Listed Dossiers

Listed Dossiers

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DRUG PRODUCT COMPOSITIONS

REF. STANDARDS OR IMPURITIES

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EDQM

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USP

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JP

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Others

PATENTS & EXCLUSIVITIES

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Health Canada Patents

DIGITAL CONTENT

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Stock Recap #PipelineProspector

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Weekly News Recap #Phispers

GLOBAL SALES INFORMATION

US Medicaid

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0RELATED EXCIPIENT COMPANIES

0EXCIPIENTS BY APPLICATIONS

Chemistry

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Also known as: 1369852-71-0, Lotilaner [inn], Credelio, Heh4938d7k, Lotilaner (ema epar: veterinary), (s)-5-[5-(3,4,5-trichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-3-methylthiophene-2-carboxylic acid [(2,2,2-trifluoroethyl carbamoyl) methyl] amide
Molecular Formula
C20H14Cl3F6N3O3S
Molecular Weight
596.8  g/mol
InChI Key
HDKWFBCPLKNOCK-SFHVURJKSA-N
FDA UNII
HEH4938D7K

Lotilaner
1 2D Structure

Lotilaner

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
3-methyl-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]-5-[(5S)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4H-1,2-oxazol-3-yl]thiophene-2-carboxamide
2.1.2 InChI
InChI=1S/C20H14Cl3F6N3O3S/c1-8-2-13(36-16(8)17(34)30-6-14(33)31-7-19(24,25)26)12-5-18(35-32-12,20(27,28)29)9-3-10(21)15(23)11(22)4-9/h2-4H,5-7H2,1H3,(H,30,34)(H,31,33)/t18-/m0/s1
2.1.3 InChI Key
HDKWFBCPLKNOCK-SFHVURJKSA-N
2.1.4 Canonical SMILES
CC1=C(SC(=C1)C2=NOC(C2)(C3=CC(=C(C(=C3)Cl)Cl)Cl)C(F)(F)F)C(=O)NCC(=O)NCC(F)(F)F
2.1.5 Isomeric SMILES
CC1=C(SC(=C1)C2=NO[C@@](C2)(C3=CC(=C(C(=C3)Cl)Cl)Cl)C(F)(F)F)C(=O)NCC(=O)NCC(F)(F)F
2.2 Other Identifiers
2.2.1 UNII
HEH4938D7K
2.3 Synonyms
2.3.1 MeSH Synonyms

1. 3-methyl-n-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl)-5-((5s)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl)-2-thiophenecarboxamide

2. Credelio

2.3.2 Depositor-Supplied Synonyms

1. 1369852-71-0

2. Lotilaner [inn]

3. Credelio

4. Heh4938d7k

5. Lotilaner (ema Epar: Veterinary)

6. (s)-5-[5-(3,4,5-trichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-3-methylthiophene-2-carboxylic Acid [(2,2,2-trifluoroethyl Carbamoyl) Methyl] Amide

7. 3-methyl-n-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]-5-[(5s)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4h-1,2-oxazol-3-yl]thiophene-2-carboxamide

8. 2-thiophenecarboxamide, 5-((5s)-4,5-dihydro-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-3-isoxazolyl)-3-methyl-n-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl)-

9. Lotilaner [usan:inn]

10. Unii-heh4938d7k

11. Lotilaner [mi]

12. Lotilaner (usan/inn)

13. Lotilaner [usan]

14. Lotilaner [green Book]

15. Chembl3707310

16. Schembl16860871

17. Dtxsid701027551

18. Ex-a3269

19. Ac-36763

20. Hy-116564

21. Cs-0065903

22. D11212

23. Q27279888

24. 3-methyi-n-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl)-5-((55)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl)thiophene-2-carboxamide

2.4 Create Date
2014-08-25
3 Chemical and Physical Properties
Molecular Weight 596.8 g/mol
Molecular Formula C20H14Cl3F6N3O3S
XLogP36.6
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count11
Rotatable Bond Count6
Exact Mass594.972565 g/mol
Monoisotopic Mass594.972565 g/mol
Topological Polar Surface Area108 Ų
Heavy Atom Count36
Formal Charge0
Complexity868
Isotope Atom Count0
Defined Atom Stereocenter Count1
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Indication

For the treatment of flea and tick infestations.

Fleas and ticks must attach to the host and commence feeding in order to be exposed to the active substance.

The veterinary medicinal product can be used as part of a treatment strategy for the control of flea allergy dermatitis (FAD).

* Dogs:

This veterinary medicinal product provides immediate and persistent killing activity for 1 month for fleas (Ctenocephalides felis and C. canis) and ticks (Rhipicephalus sanguineus, Ixodes ricinus, I. hexagonus and Dermacentor reticulatus).

* Cats:

This veterinary medicinal product provides immediate and persistent killing activity for 1 month against fleas (Ctenocephalides felis and C. canis) and ticks (Ixodes ricinus).


5 Pharmacology and Biochemistry
5.1 ATC Code

QP53BE04


API SUPPLIERS

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01

Metrochem API Private Limited

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

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Medlab Asia & Asia Health
Not Confirmed
  • fda
  • EDQM
  • WHO-GMP

Virtual BoothMetrochem has been delivering customized volume & quality products to customers across the world, taking utmost care of their needs.

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USDMF CEP/COS JDMF EU-WC NDC KDMF VMF Others AUDIT
Metrochem

02

Shandong Chenghui Shuangda Pharmac...

China

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothShuangda Pharmaceutical has a world-class first-class production line, having GMP, FDA and other regulatory certifications.

Flag China
Digital Content Digital Content
USDMF CEP/COS JDMF EU-WC NDC KDMF VMF Others AUDIT
Shandong Chenghui Shuangda Pharmaceutical

03

Alivira Animal Health

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

Medlab Asia & Asia Health
Not Confirmed
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Alivira Animal Health

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

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Medlab Asia & Asia Health
Not Confirmed
USDMF CEP/COS JDMF EU-WC NDC KDMF VMF Others AUDIT
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05

Alembic Pharmaceuticals Limited

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

Medlab Asia & Asia Health
Not Confirmed
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NDC API

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01

Siegfried AG

Switzerland
AES 2024
Not Confirmed
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Siegfried AG

Switzerland
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AES 2024
Not Confirmed

LOTILANER

NDC Package Code : 17205-629

Start Marketing Date : 2023-08-14

End Marketing Date : 2025-12-31

Dosage Form (Strength) : POWDER (1kg/kg)

Marketing Category : BULK INGREDIENT

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Listed Suppliers

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01

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AES 2024
Not Confirmed
  • fda
  • EDQM
  • WHO-GMP

Virtual BoothMetrochem has been delivering customized volume & quality products to customers across the world, taking utmost care of their needs.

Flag India
Digital Content Digital Content

Lotilaner

About the Company :

Established in 2004, Metrochem API is one of the fastest-growing APIs, pellets & intermediates manufacturers. It has 6 dedicated manufacturing facilities for its 3 core product ...

Established in 2004, Metrochem API is one of the fastest-growing APIs, pellets & intermediates manufacturers. It has 6 dedicated manufacturing facilities for its 3 core product groups and has been approved by ISO 9001-2015, USFDA, WHO GMP, Cofepris & Japanese authorities. Metrochem’s in-depth industry knowledge, & hi-tech & advanced infrastructure, helps it provide quality products to its customers. Note: None of the products will be supplied to the countries where this could conflict with existing patents. Further, any products under patent will be offered for R&D purposes only. However, the final responsibility lies with the buyer
Metrochem

02

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothShuangda Pharmaceutical has a world-class first-class production line, having GMP, FDA and other regulatory certifications.

Flag China
Digital Content Digital Content

Lotilaner

About the Company : Shandong Chenghui Shuangda Pharmaceutical Co., Ltd. is specialized in R&D and production of APIs and advanced intermediates. With 22 years of production experience,the company has ...

Shandong Chenghui Shuangda Pharmaceutical Co., Ltd. is specialized in R&D and production of APIs and advanced intermediates. With 22 years of production experience,the company has 6 workshops and 9 production lines which has 100t/month production capacity.The company is committed to maintain the standards with continuous improvements to the current standards throughout the product lifecycle.The main products include local anesthetic drugs, antiviral drugs, cardiovascular and cerebrovascular drugs, antitumor drugs, gastrointestinal drugs, diabetic drugs, veterinary drugs, and CDMO products.
Shandong Chenghui Shuangda Pharmaceutical

03

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  • EDQM
  • WHO-GMP

Virtual BoothTAPI offers customized CDMO Solutions for API development and manufacturing services.

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Digital Content Digital Content

Lotilaner

About the Company : Founded in 1935, TAPI Technology & API Services has a long-standing tradition of advancing health through innovation and dedication. Today, we proudly build upon this legacy, drivi...

Founded in 1935, TAPI Technology & API Services has a long-standing tradition of advancing health through innovation and dedication. Today, we proudly build upon this legacy, driving progress in the pharmaceutical industry. Leveraging our extensive experience and world-class expertise, we deliver one of the most comprehensive API portfolios in the industry. Additionally, we provide tailored CDMO services, harnessing our proficiency in diverse technologies to meet our partners' unique needs, ensuring flexibility and excellence in every project.
TAPI Company Banner

04

AES 2024
Not Confirmed
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AES 2024
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Lotilaner

About the Company : Alembic Pharmaceuticals Limited is a leading pharmaceutical company in India. The Company is vertically integrated with the ability to develop, manufacture and market pharmaceutica...

Alembic Pharmaceuticals Limited is a leading pharmaceutical company in India. The Company is vertically integrated with the ability to develop, manufacture and market pharmaceutical products, pharmaceutical substances and Intermediates.
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05

AES 2024
Not Confirmed
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AES 2024
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Lotilaner

About the Company : Alivira Animal Health Limited has emerged as India's largest and 1st Global integrated animal health company specialising in manufacturing of Active Pharmaceutical Ingredients (API...

Alivira Animal Health Limited has emerged as India's largest and 1st Global integrated animal health company specialising in manufacturing of Active Pharmaceutical Ingredients (API) and Finished Dosage Formulations (FDF).Our logotype is inspired by nature and its different forms and shapes. From a microscopic view to the skin texture, footprint of a chosen animal. The circular shape evokes the idea of protection and control. It’s a closed and perfect shape that is naturally balanced, reminiscing the brand idea “Animals source of health.
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Drugs in Development

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Details:

Proceeds will be used for the U.S. commercialization of Xdemy (lotilaner), designed to target and kill Demodex mites causing Demodex blepharitis.


Lead Product(s): Lotilaner

Therapeutic Area: Ophthalmology Brand Name: Xdemvy

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Goldman Sachs & Co. LLC

Deal Size: $100.0 million Upfront Cash: Undisclosed

Deal Type: Public Offering February 29, 2024

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01

AES 2024
Not Confirmed
AES 2024
Not Confirmed

Lead Product(s) : Lotilaner

Therapeutic Area : Ophthalmology

Highest Development Status : Approved

Partner/Sponsor/Collaborator : Goldman Sachs & Co. LLC

Deal Size : $100.0 million

Deal Type : Public Offering

Details : Proceeds will be used for the U.S. commercialization of Xdemy (lotilaner), designed to target and kill Demodex mites causing Demodex blepharitis.

Brand Name : Xdemvy

Molecule Type : Small molecule

Upfront Cash : Undisclosed

February 29, 2024

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Details:

TP-05 (lotilaner) is an oral, well-characterized anti-parasitic agent that selectively inhibits parasite-specific GABA-Cl channels. It is being evaluated for the prevention of Lyme Disease.


Lead Product(s): Lotilaner

Therapeutic Area: Infections and Infectious Diseases Brand Name: TP-05

Study Phase: Phase IIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable February 22, 2024

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02

AES 2024
Not Confirmed
AES 2024
Not Confirmed

Details : TP-05 (lotilaner) is an oral, well-characterized anti-parasitic agent that selectively inhibits parasite-specific GABA-Cl channels. It is being evaluated for the prevention of Lyme Disease.

Brand Name : TP-05

Molecule Type : Small molecule

Upfront Cash : Not Applicable

February 22, 2024

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Details:

TP-03 (lotilaner ophthalmic solution, 0.25%) is a novel small molecule, approved for Demodex blepharitis under the brand name Xdemvy. Now it is being evaluated as an investigational therapy for the treatment of Meibomian Gland Disease (MGD) in patients with Demodex mites.


Lead Product(s): Lotilaner

Therapeutic Area: Ophthalmology Brand Name: TP-03

Study Phase: Phase IIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable December 11, 2023

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03

AES 2024
Not Confirmed
AES 2024
Not Confirmed

Details : TP-03 (lotilaner ophthalmic solution, 0.25%) is a novel small molecule, approved for Demodex blepharitis under the brand name Xdemvy. Now it is being evaluated as an investigational therapy for the treatment of Meibomian Gland Disease (MGD) in patients w...

Brand Name : TP-03

Molecule Type : Small molecule

Upfront Cash : Not Applicable

December 11, 2023

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Details:

TP-03 (lotilaner) is a novel investigational therapeutic designed to resolve the signs and symptoms of Demodex blepharitis via targeting and eradicating the root cause by selectively inhibiting the GABA-Cl channels.


Lead Product(s): Lotilaner

Therapeutic Area: Ophthalmology Brand Name: TP-03

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable October 30, 2023

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04

LianBio

China
arrow
AES 2024
Not Confirmed

LianBio

China
arrow
AES 2024
Not Confirmed

Details : TP-03 (lotilaner) is a novel investigational therapeutic designed to resolve the signs and symptoms of Demodex blepharitis via targeting and eradicating the root cause by selectively inhibiting the GABA-Cl channels.

Brand Name : TP-03

Molecule Type : Small molecule

Upfront Cash : Not Applicable

October 30, 2023

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Details:

The company intends to use the net proceeds to fund the commercial launch of Xdemvy (lotilaner) for the treatment of Demodex blepharitis in the United States and to develop its product pipeline including TP-03 for the treatment of Meibomian Gland Disease.


Lead Product(s): Lotilaner

Therapeutic Area: Ophthalmology Brand Name: Xdemvy

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Goldman Sachs & Co. LLC

Deal Size: $100.0 million Upfront Cash: Undisclosed

Deal Type: Public Offering August 01, 2023

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05

AES 2024
Not Confirmed
AES 2024
Not Confirmed

Lead Product(s) : Lotilaner

Therapeutic Area : Ophthalmology

Highest Development Status : Approved

Partner/Sponsor/Collaborator : Goldman Sachs & Co. LLC

Deal Size : $100.0 million

Deal Type : Public Offering

Details : The company intends to use the net proceeds to fund the commercial launch of Xdemvy (lotilaner) for the treatment of Demodex blepharitis in the United States and to develop its product pipeline including TP-03 for the treatment of Meibomian Gland Disease...

Brand Name : Xdemvy

Molecule Type : Small molecule

Upfront Cash : Undisclosed

August 01, 2023

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Details:

The company intends to fund the commercial launch of Xdemvy (lotilaner) for the treatment of Demodex blepharitis in the United States and to develop its product pipeline including TP-03 for the treatment of Meibomian Gland Disease, or MGD, TP-04 and TP-05.


Lead Product(s): Lotilaner

Therapeutic Area: Ophthalmology Brand Name: Xdemvy

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Goldman Sachs & Co. LLC

Deal Size: $100.0 million Upfront Cash: Undisclosed

Deal Type: Public Offering July 31, 2023

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06

AES 2024
Not Confirmed
AES 2024
Not Confirmed

Lead Product(s) : Lotilaner

Therapeutic Area : Ophthalmology

Highest Development Status : Approved

Partner/Sponsor/Collaborator : Goldman Sachs & Co. LLC

Deal Size : $100.0 million

Deal Type : Public Offering

Details : The company intends to fund the commercial launch of Xdemvy (lotilaner) for the treatment of Demodex blepharitis in the United States and to develop its product pipeline including TP-03 for the treatment of Meibomian Gland Disease, or MGD, TP-04 and TP-0...

Brand Name : Xdemvy

Molecule Type : Small molecule

Upfront Cash : Undisclosed

July 31, 2023

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Details:

Xdemvy (lotilaner ophthalmic solution), a novel prescription eye drop, is recently approved by FDA and is designed to treat demodex blepharitis by targeting and eradicating the root cause of the disease, demodex mite infestation.


Lead Product(s): Lotilaner

Therapeutic Area: Ophthalmology Brand Name: Xdemvy

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable July 25, 2023

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07

AES 2024
Not Confirmed
AES 2024
Not Confirmed

Details : Xdemvy (lotilaner ophthalmic solution), a novel prescription eye drop, is recently approved by FDA and is designed to treat demodex blepharitis by targeting and eradicating the root cause of the disease, demodex mite infestation.

Brand Name : Xdemvy

Molecule Type : Small molecule

Upfront Cash : Not Applicable

July 25, 2023

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Details:

TP-03 (lotilaner) is a novel investigational therapeutic designed to resolve the signs and symptoms of Demodex blepharitis by targeting and eradicating the root cause of the demodex mite infestation.


Lead Product(s): Lotilaner

Therapeutic Area: Ophthalmology Brand Name: TP-03

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Tarsus Pharmaceuticals

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable June 08, 2023

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08

LianBio

China
arrow
AES 2024
Not Confirmed

LianBio

China
arrow
AES 2024
Not Confirmed

Details : TP-03 (lotilaner) is a novel investigational therapeutic designed to resolve the signs and symptoms of Demodex blepharitis by targeting and eradicating the root cause of the demodex mite infestation.

Brand Name : TP-03

Molecule Type : Small molecule

Upfront Cash : Not Applicable

June 08, 2023

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Details:

TP-05 is an oral systemic formulation of lotilaner, a well-characterized anti-parasitic agent that paralyzes and kills ticks that transmit Lyme disease by selectively inhibiting parasite-specific GABA-CI channels.


Lead Product(s): Lotilaner

Therapeutic Area: Infections and Infectious Diseases Brand Name: TP-05

Study Phase: Phase IIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable December 15, 2022

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09

AES 2024
Not Confirmed
AES 2024
Not Confirmed

Details : TP-05 is an oral systemic formulation of lotilaner, a well-characterized anti-parasitic agent that paralyzes and kills ticks that transmit Lyme disease by selectively inhibiting parasite-specific GABA-CI channels.

Brand Name : TP-05

Molecule Type : Small molecule

Upfront Cash : Not Applicable

December 15, 2022

blank

Details:

TP-03 (lotilaner ophthalmic solution, 0.25%) is a novel, investigational therapeutic designed to resolve the signs of Demodex blepharitis by targeting and eradicating the root cause of the disease – Demodex mite infestation.


Lead Product(s): Lotilaner

Therapeutic Area: Ophthalmology Brand Name: TP-03

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable November 01, 2022

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10

LianBio

China
arrow
AES 2024
Not Confirmed

LianBio

China
arrow
AES 2024
Not Confirmed

Details : TP-03 (lotilaner ophthalmic solution, 0.25%) is a novel, investigational therapeutic designed to resolve the signs of Demodex blepharitis by targeting and eradicating the root cause of the disease – Demodex mite infestation.

Brand Name : TP-03

Molecule Type : Small molecule

Upfront Cash : Not Applicable

November 01, 2022

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INTERMEDIATES SUPPLIERS

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01

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothShuangda Pharmaceutical has a world-class first-class production line, having GMP, FDA and other regulatory certifications.

CAS Number : 859199-06-7

End Use API : Lotilaner

About The Company : Shandong Chenghui Shuangda Pharmaceutical Co., Ltd. is specialized in R&D and production of APIs and advanced intermediates. With 22 years of production experie...

Shandong Chenghui Shuangda Pharmaceutical

02

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothShuangda Pharmaceutical has a world-class first-class production line, having GMP, FDA and other regulatory certifications.

CAS Number : 2758907-87-6

End Use API : Lotilaner

About The Company : Shandong Chenghui Shuangda Pharmaceutical Co., Ltd. is specialized in R&D and production of APIs and advanced intermediates. With 22 years of production experie...

Shandong Chenghui Shuangda Pharmaceutical

03

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothShuangda Pharmaceutical has a world-class first-class production line, having GMP, FDA and other regulatory certifications.

CAS Number : 158401-00-4

End Use API : Lotilaner

About The Company : Shandong Chenghui Shuangda Pharmaceutical Co., Ltd. is specialized in R&D and production of APIs and advanced intermediates. With 22 years of production experie...

Shandong Chenghui Shuangda Pharmaceutical
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