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Also known as: 1223405-08-0, Loxo-101 sulfate, Arry-470 sulfate, Loxo-101 (sulfate), (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide sulfate, Rdf76r62id
Molecular Formula
C21H24F2N6O6S
Molecular Weight
526.5  g/mol
InChI Key
PXHANKVTFWSDSG-QLOBERJESA-N
FDA UNII
RDF76R62ID

Larotrectinib Sulfate
Larotrectinib Sulfate is the sulfate salt form of larotrectinib, an orally available, tropomyosin receptor kinase (Trk) inhibitor, with potential antineoplastic activity. Upon administration, larotrectinib binds to Trk, thereby preventing neurotrophin-Trk interaction and Trk activation, which results in both the induction of cellular apoptosis and the inhibition of cell growth in tumors that overexpress Trk. Trk, a receptor tyrosine kinase activated by neurotrophins, is mutated in a variety of cancer cell types and plays an important role in tumor cell growth and survival.
1 2D Structure

Larotrectinib Sulfate

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
(3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxypyrrolidine-1-carboxamide;sulfuric acid
2.1.2 InChI
InChI=1S/C21H22F2N6O2.H2O4S/c22-13-3-4-16(23)15(10-13)18-2-1-7-28(18)19-6-9-29-20(26-19)17(11-24-29)25-21(31)27-8-5-14(30)12-27;1-5(2,3)4/h3-4,6,9-11,14,18,30H,1-2,5,7-8,12H2,(H,25,31);(H2,1,2,3,4)/t14-,18+;/m0./s1
2.1.3 InChI Key
PXHANKVTFWSDSG-QLOBERJESA-N
2.1.4 Canonical SMILES
C1CC(N(C1)C2=NC3=C(C=NN3C=C2)NC(=O)N4CCC(C4)O)C5=C(C=CC(=C5)F)F.OS(=O)(=O)O
2.1.5 Isomeric SMILES
C1C[C@@H](N(C1)C2=NC3=C(C=NN3C=C2)NC(=O)N4CC[C@@H](C4)O)C5=C(C=CC(=C5)F)F.OS(=O)(=O)O
2.2 Other Identifiers
2.2.1 UNII
RDF76R62ID
2.3 Synonyms
2.3.1 MeSH Synonyms

1. (3s)-n-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide

2. Arry-470

3. Arry470

4. Bay-2757556

5. Bay2757556

6. Larotrectinib

7. Loxo-101

8. Loxo101

9. N-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide

10. Vitrakvi

2.3.2 Depositor-Supplied Synonyms

1. 1223405-08-0

2. Loxo-101 Sulfate

3. Arry-470 Sulfate

4. Loxo-101 (sulfate)

5. (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide Sulfate

6. Rdf76r62id

7. Larotrectinib Sulfate [usan]

8. Vitrakvi

9. (3s)-n-[5-[(2r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxypyrrolidine-1-carboxamide;sulfuric Acid

10. 1-pyrrolidinecarboxamide, N-(5-((2r)-2-(2,5-difluorophenyl)-1-pyrrolidinyl)pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxy-, (3s)-, Sulfate (1:1)

11. Vitrakvi (tn)

12. 1-pyrrolidinecarboxamide, N-[5-[(2r)-2-(2,5-difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-, (3s)-, Sulfate (1:1)

13. Larotrectinib (loxo-101) Sulfate

14. Larotrectinib Sulphate

15. Loxo-101(sulfate)

16. Arry-470 (sulfate)

17. Unii-rdf76r62id

18. Schembl2239598

19. Chembl3989939

20. Ex-a1981a

21. Dtxsid401026485

22. Hms3886n19

23. Larotrectinib Sulfate (jan/usan)

24. Larotrectinib Sulfate [mi]

25. Larotrectinib Sulfate [jan]

26. Amy12423

27. Larotrectinib (loxo-101 Sulfate)

28. Hy-12866a

29. Mfcd29472286

30. S7960

31. Larotrectinib Sulfate [who-dd]

32. Ccg-269890

33. Cs-5314

34. Ac-30671

35. Bl161518

36. Larotrectinib Sulfate [orange Book]

37. D11138

38. (3s)-n-(5-((2r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide Sulfate (1:1)

39. (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide Hydrogen Sulfate

2.4 Create Date
2012-11-30
3 Chemical and Physical Properties
Molecular Weight 526.5 g/mol
Molecular Formula C21H24F2N6O6S
Hydrogen Bond Donor Count4
Hydrogen Bond Acceptor Count11
Rotatable Bond Count3
Exact Mass526.14461000 g/mol
Monoisotopic Mass526.14461000 g/mol
Topological Polar Surface Area169 Ų
Heavy Atom Count36
Formal Charge0
Complexity741
Isotope Atom Count0
Defined Atom Stereocenter Count2
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count2
4 Drug and Medication Information
4.1 Drug Indication

Vitrakvi as monotherapy is indicated for the treatment of adult and paediatric patients with solid tumours that display a Neurotrophic Tyrosine Receptor Kinase (NTRK) gene fusion,

- who have a disease that is locally advanced, metastatic or where surgical resection is likely to result in severe morbidity, and

- who have no satisfactory treatment options.


5 Pharmacology and Biochemistry
5.1 ATC Code

L01XE53


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LAROTRECTINIB SULFATE

NDC Package Code : 22568-1752

Start Marketing Date : 2021-06-01

End Marketing Date : 2025-12-31

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

Marketing Category : BULK INGREDIENT

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LAROTRECTINIB SULFATE

NDC Package Code : 17337-0324

Start Marketing Date : 2023-04-21

End Marketing Date : 2025-12-31

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

Marketing Category : BULK INGREDIENT

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LAROTRECTINIB SULFATE

NDC Package Code : 17337-0317

Start Marketing Date : 2022-07-11

End Marketing Date : 2025-12-31

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

Marketing Category : BULK INGREDIENT

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LAROTRECTINIB SULFATE

NDC Package Code : 17337-0316

Start Marketing Date : 2022-06-08

End Marketing Date : 2025-12-31

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

Marketing Category : BULK INGREDIENT

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Larotrectinib Sulfate

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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Larotrectinib Sulfate

About the Company : Beijing Sjar Technology Development Co., Ltd. founded in 2014, it is a high-tech enterprise which specialized in the research and development of active pharmaceutical ingredients a...

Beijing Sjar Technology Development Co., Ltd. founded in 2014, it is a high-tech enterprise which specialized in the research and development of active pharmaceutical ingredients and their intermediates, electronic chemical materials and intermediates, large-scale production, sales and services, and provide customized synthetic services according to customer requirements. Sjar-Tech locates in Beijing Economic and Technological Development Zone, has its own R&D and development laboratory. Sjar-Tech has set up a R&D team with rich experience and strong technical strength, most of the practitioners have more than ten years' experience.
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Larotrectinib Sulfate

About the Company : Hope Chem is dedicated to manufacturing, marketing, and CMO service of Active Pharmaceutical Ingredients (APIs), Intermediates, and Specialty Chemicals since the year 2010. Current...

Hope Chem is dedicated to manufacturing, marketing, and CMO service of Active Pharmaceutical Ingredients (APIs), Intermediates, and Specialty Chemicals since the year 2010. Currently, they have exclusive partnerships with multiple, state-of-the-art and GMP-compliant manufacturers in China and abroad to service our esteemed partners for competitive, long-term & stable supplies. The main products are APIs and intermediates of antiviral drug substances and anti-inflammatory, analgesic, and non-steroidal pharmaceuticals.
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05-Jun-2021
08-Oct-2024
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Drugs in Development

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Details:

Vitrakvi (larotrectinib sulfate) is an inhibitor of the TRKA, TRKB, and TRKC. It is approved for the treatment of adult and pediatric patients with ntrk gene fusion-positive solid tumors.


Lead Product(s): Larotrectinib Sulfate

Therapeutic Area: Oncology Brand Name: Vitrakvi

Study Phase: Approved FDFProduct Type: Other Small Molecule

Sponsor: Inapplicable

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable April 10, 2025

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Bayer AG

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Details : Vitrakvi (larotrectinib sulfate) is an inhibitor of the TRKA, TRKB, and TRKC. It is approved for the treatment of adult and pediatric patients with ntrk gene fusion-positive solid tumors.

Product Name : Vitrakvi

Product Type : Other Small Molecule

Upfront Cash : Inapplicable

April 10, 2025

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LAROTRECTINIB SULFATE

Brand Name : VITRAKVI

Dosage Form : CAPSULE;ORAL

Dosage Strength : EQ 25MG BASE

Packaging :

Approval Date : 2018-11-26

Application Number : 210861

Regulatory Info : RX

Registration Country : USA

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LAROTRECTINIB SULFATE

Brand Name : VITRAKVI

Dosage Form : CAPSULE;ORAL

Dosage Strength : EQ 100MG BASE

Packaging :

Approval Date : 2018-11-26

Application Number : 210861

Regulatory Info : RX

Registration Country : USA

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LAROTRECTINIB SULFATE

Brand Name : VITRAKVI

Dosage Form : SOLUTION;ORAL

Dosage Strength : EQ 20MG BASE/ML

Packaging :

Approval Date : 2018-11-26

Application Number : 211710

Regulatory Info : RX

Registration Country : USA

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LAROTRECTINIB SULFATE

Brand Name : VITRAKVI

Dosage Form : CAPSULE;ORAL

Dosage Strength : EQ 25MG BASE

Approval Date : 2018-11-26

Application Number : 210861

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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BAYER HLTHCARE

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LAROTRECTINIB SULFATE

Brand Name : VITRAKVI

Dosage Form : CAPSULE;ORAL

Dosage Strength : EQ 100MG BASE

Approval Date : 2018-11-26

Application Number : 210861

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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LAROTRECTINIB SULFATE

Brand Name : VITRAKVI

Dosage Form : SOLUTION;ORAL

Dosage Strength : EQ 20MG BASE/ML

Approval Date : 2018-11-26

Application Number : 211710

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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Patents & EXCLUSIVITIES

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US Patents

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LAROTRECTINIB SULFATE

US Patent Number : 11337967

Drug Substance Claim :

Drug Product Claim :

Application Number : 210861

Patent Use Code : U-4123

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2037-05-16

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LAROTRECTINIB SULFATE

US Patent Number : 9676783

Drug Substance Claim :

Drug Product Claim :

Application Number : 210861

Patent Use Code : U-2469

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2029-10-21

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LAROTRECTINIB SULFATE

US Patent Number : 10172861

Drug Substance Claim : Y

Drug Product Claim :

Application Number : 211710

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2035-11-16

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LAROTRECTINIB SULFATE

US Patent Number : 10045991

Drug Substance Claim :

Drug Product Claim :

Application Number : 211710

Patent Use Code : U-2473

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2037-04-04

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LAROTRECTINIB SULFATE

US Patent Number : 10799505

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 210861

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2036-08-15

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LAROTRECTINIB SULFATE

US Patent Number : 11974998

Drug Substance Claim :

Drug Product Claim :

Application Number : 211710

Patent Use Code : U-4124

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2037-05-16

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LAROTRECTINIB SULFATE

US Patent Number : 10285993

Drug Substance Claim :

Drug Product Claim :

Application Number : 210861

Patent Use Code : U-2470

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2035-11-16

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LAROTRECTINIB SULFATE

US Patent Number : 9127013

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 211710

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2029-10-21

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LAROTRECTINIB SULFATE

US Patent Number : 9782414

Drug Substance Claim :

Drug Product Claim :

Application Number : 211710

Patent Use Code : U-2471

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2035-11-16

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LAROTRECTINIB SULFATE

US Patent Number : 8513263

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 211710

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2029-12-23

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US Exclusivities

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BAYER HLTHCARE

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LAROTRECTINIB SULFATE

Exclusivity Code : ODE-215

Exclusivity Expiration Date : 2025-11-26

Application Number : 210861

Product Number : 1

Exclusivity Details :

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BAYER HLTHCARE

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LAROTRECTINIB SULFATE

Exclusivity Code : ODE-220

Exclusivity Expiration Date : 2025-11-26

Application Number : 210861

Product Number : 1

Exclusivity Details :

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LAROTRECTINIB SULFATE

Exclusivity Code : ODE-221

Exclusivity Expiration Date : 2025-11-26

Application Number : 210861

Product Number : 1

Exclusivity Details :

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BAYER HLTHCARE

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LAROTRECTINIB SULFATE

Exclusivity Code : ODE-215

Exclusivity Expiration Date : 2025-11-26

Application Number : 210861

Product Number : 2

Exclusivity Details :

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LAROTRECTINIB SULFATE

Exclusivity Code : ODE-220

Exclusivity Expiration Date : 2025-11-26

Application Number : 210861

Product Number : 2

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BAYER HLTHCARE

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LAROTRECTINIB SULFATE

Exclusivity Code : ODE-221

Exclusivity Expiration Date : 2025-11-26

Application Number : 210861

Product Number : 2

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LAROTRECTINIB SULFATE

Exclusivity Code : ODE-215

Exclusivity Expiration Date : 2025-11-26

Application Number : 211710

Product Number : 1

Exclusivity Details :

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LAROTRECTINIB SULFATE

Exclusivity Code : ODE-220

Exclusivity Expiration Date : 2025-11-26

Application Number : 211710

Product Number : 1

Exclusivity Details :

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Iran Expo
Not Confirmed
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Exclusivity Code : ODE-221

Exclusivity Expiration Date : 2025-11-26

Application Number : 211710

Product Number : 1

Exclusivity Details :

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ABOUT THIS PAGE

Looking for 1223405-08-0 / Larotrectinib Sulfate API manufacturers, exporters & distributors?

Larotrectinib Sulfate manufacturers, exporters & distributors 1

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PharmaCompass offers a list of Larotrectinib Sulfate API manufacturers, exporters & distributors, which can be sorted by GMP, USDMF, JDMF, KDMF, CEP (COS), WC, Price,and more, enabling you to easily find the right Larotrectinib Sulfate manufacturer or Larotrectinib Sulfate supplier for your needs.

Send us enquiries for free, and we will assist you in establishing a direct connection with your preferred Larotrectinib Sulfate manufacturer or Larotrectinib Sulfate supplier.

PharmaCompass also assists you with knowing the Larotrectinib Sulfate API Price utilized in the formulation of products. Larotrectinib Sulfate API Price is not always fixed or binding as the Larotrectinib Sulfate Price is obtained through a variety of data sources. The Larotrectinib Sulfate Price can also vary due to multiple factors, including market conditions, regulatory modifications, or negotiated pricing deals.

API | Excipient name

Larotrectinib Sulfate

Synonyms

1223405-08-0, Loxo-101 sulfate, Arry-470 sulfate, Loxo-101 (sulfate), (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide sulfate, Rdf76r62id

Cas Number

1223405-08-0

Unique Ingredient Identifier (UNII)

RDF76R62ID

About Larotrectinib Sulfate

Larotrectinib Sulfate is the sulfate salt form of larotrectinib, an orally available, tropomyosin receptor kinase (Trk) inhibitor, with potential antineoplastic activity. Upon administration, larotrectinib binds to Trk, thereby preventing neurotrophin-Trk interaction and Trk activation, which results in both the induction of cellular apoptosis and the inhibition of cell growth in tumors that overexpress Trk. Trk, a receptor tyrosine kinase activated by neurotrophins, is mutated in a variety of cancer cell types and plays an important role in tumor cell growth and survival.

Larotrectinib Sulfate Manufacturers

A Larotrectinib Sulfate manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Larotrectinib Sulfate, including repackagers and relabelers. The FDA regulates Larotrectinib Sulfate manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Larotrectinib Sulfate API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.

click here to find a list of Larotrectinib Sulfate manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.

Larotrectinib Sulfate Suppliers

A Larotrectinib Sulfate supplier is an individual or a company that provides Larotrectinib Sulfate active pharmaceutical ingredient (API) or Larotrectinib Sulfate finished formulations upon request. The Larotrectinib Sulfate suppliers may include Larotrectinib Sulfate API manufacturers, exporters, distributors and traders.

click here to find a list of Larotrectinib Sulfate suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.

Larotrectinib Sulfate USDMF

A Larotrectinib Sulfate DMF (Drug Master File) is a document detailing the whole manufacturing process of Larotrectinib Sulfate active pharmaceutical ingredient (API) in detail. Different forms of Larotrectinib Sulfate DMFs exist exist since differing nations have different regulations, such as Larotrectinib Sulfate USDMF, ASMF (EDMF), JDMF, CDMF, etc.

A Larotrectinib Sulfate DMF submitted to regulatory agencies in the US is known as a USDMF. Larotrectinib Sulfate USDMF includes data on Larotrectinib Sulfate's chemical properties, information on the facilities and procedures used, and details about packaging and storage. The Larotrectinib Sulfate USDMF is kept confidential to protect the manufacturer’s intellectual property.

click here to find a list of Larotrectinib Sulfate suppliers with USDMF on PharmaCompass.

Larotrectinib Sulfate NDC

National Drug Code is a comprehensive database maintained by the FDA that contains information on all drugs marketed in the US. This directory includes information about finished drug products, unfinished drug products, and compounded drug products, including those containing Larotrectinib Sulfate as an active pharmaceutical ingredient (API).

Finished drug products

The FDA updates the NDC directory daily. The NDC numbers for Larotrectinib Sulfate API and other APIs are published in this directory by the FDA.

Unfinished drugs

The NDC unfinished drugs database includes product listing information submitted for all unfinished drugs, such as active pharmaceutical ingredients (APIs), drugs intended for further processing and bulk drug substances for compounding.

Pharmaceutical companies that manufacture Larotrectinib Sulfate as an active pharmaceutical ingredient (API) must furnish the FDA with an updated record of all drugs that they produce, prepare, propagate, compound, or process for commercial distribution in the US at their facilities.

Compounded drug products

The NDC directory also contains data on finished compounded human drug products that contain Larotrectinib Sulfate and are produced by outsourcing facilities. While these outsourcing facilities are not mandated to assign a Larotrectinib Sulfate NDC to their finished compounded human drug products, they may choose to do so.

click here to find a list of Larotrectinib Sulfate suppliers with NDC on PharmaCompass.

Larotrectinib Sulfate GMP

Larotrectinib Sulfate Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.

GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).

PharmaCompass offers a list of Larotrectinib Sulfate GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, API price, and more, enabling you to easily find the right Larotrectinib Sulfate GMP manufacturer or Larotrectinib Sulfate GMP API supplier for your needs.

Larotrectinib Sulfate CoA

A Larotrectinib Sulfate CoA (Certificate of Analysis) is a formal document that attests to Larotrectinib Sulfate's compliance with Larotrectinib Sulfate specifications and serves as a tool for batch-level quality control.

Larotrectinib Sulfate CoA mostly includes findings from lab analyses of a specific batch. For each Larotrectinib Sulfate CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.

Larotrectinib Sulfate may be tested according to a variety of international standards, such as European Pharmacopoeia (Larotrectinib Sulfate EP), Larotrectinib Sulfate JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Larotrectinib Sulfate USP).

Inform the supplier about your product requirements, specifying if you need a product with particular monograph like EP (Ph. Eur.), USP, JP, BP, or any other quality. In addition, clarify whether you need hydrochloride (HCl), anhydricum, base, micronisatum or a specific level of purity. To find reputable suppliers, utilize the filters and select those certified by GMP, FDA, or any other certification as per your requirement.
For your convenience, we have listed synonyms and CAS numbers to help you find the best supplier. The use of synonyms and CAS numbers can be helpful in identifying potential suppliers, but it is crucial to note that they might not always indicate the exact same product. It is important to confirm the product details with the supplier before making a purchase to ensure that it meets your requirements.
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