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Chemistry

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Also known as: Resiniferatoxin, Chembl448382, Bdbm50366620
Molecular Formula
C37H40O9
Molecular Weight
628.7  g/mol
InChI Key
DSDNAKHZNJAGHN-GGIHZKEUSA-N

Resiniferatoxin
Resiniferatoxin is a naturally occurring capsaicin analog found in the latex of the cactus Euphorbia resinifera with analgesic activity. Resiniferatoxin (RTX) binds to and activates the transient receptor potential vanilloid 1 (TRPV1), a non-selective cation channel in the plasma membrane of primary afferent sensory neurons. This increases the permeability to cations, and leads to an influx of calcium and sodium ions. This results in membrane depolarization, causing an irritant effect, followed by desensitization of the sensory neurons thereby inhibiting signal conduction in afferent pain pathways and causing analgesia. TRPV1, a member of the transient receptor potential channel (TRP) superfamily, is a heat- and chemo-sensitive calcium/sodium ion channel that is selectively expressed in a subpopulation of pain-sensing primary afferent neurons.
1 2D Structure

Resiniferatoxin

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
[(1R,2R,6R,10S,11R,15S,17R)-13-benzyl-6-hydroxy-4,17-dimethyl-5-oxo-15-prop-1-en-2-yl-12,14,18-trioxapentacyclo[11.4.1.01,10.02,6.011,15]octadeca-3,8-dien-8-yl]methyl 2-(4-hydroxy-3-methoxyphenyl)acetate
2.1.2 InChI
InChI=1S/C37H40O9/c1-21(2)35-17-23(4)37-27(33(35)44-36(45-35,46-37)19-24-9-7-6-8-10-24)14-26(18-34(41)30(37)13-22(3)32(34)40)20-43-31(39)16-25-11-12-28(38)29(15-25)42-5/h6-15,23,27,30,33,38,41H,1,16-20H2,2-5H3/t23-,27+,30-,33-,34-,35+,36?,37-/m1/s1
2.1.3 InChI Key
DSDNAKHZNJAGHN-GGIHZKEUSA-N
2.1.4 Canonical SMILES
CC1CC2(C3C4C1(C5C=C(C(=O)C5(CC(=C4)COC(=O)CC6=CC(=C(C=C6)O)OC)O)C)OC(O3)(O2)CC7=CC=CC=C7)C(=C)C
2.1.5 Isomeric SMILES
C[C@@H]1C[C@@]2([C@H]3[C@H]4[C@]1([C@@H]5C=C(C(=O)[C@]5(CC(=C4)COC(=O)CC6=CC(=C(C=C6)O)OC)O)C)OC(O3)(O2)CC7=CC=CC=C7)C(=C)C
2.2 Synonyms
2.2.1 MeSH Synonyms

1. Reciniferatoxin

2. Resiniferatoxin

3. Rtx Diterpene

2.2.2 Depositor-Supplied Synonyms

1. Resiniferatoxin

2. Chembl448382

3. Bdbm50366620

2.3 Create Date
2010-01-26
3 Chemical and Physical Properties
Molecular Weight 628.7 g/mol
Molecular Formula C37H40O9
XLogP34.5
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count9
Rotatable Bond Count9
Exact Mass628.26723285 g/mol
Monoisotopic Mass628.26723285 g/mol
Topological Polar Surface Area121 Ų
Heavy Atom Count46
Formal Charge0
Complexity1330
Isotope Atom Count0
Defined Atom Stereocenter Count7
Undefined Atom Stereocenter Count1
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1

API SUPPLIERS

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Drugs in Development

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Details:

RTX (resiniferatoxin) is a small molecule which is act as TRPV1 agonist, which is investigated for the treatment of knee pain in moderate to severe osteoarthritis of the knee (OAK) patients.


Lead Product(s): Resiniferatoxin

Therapeutic Area: Musculoskeletal Brand Name: RTX

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable September 07, 2023

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01

Duphat
Not Confirmed
Duphat
Not Confirmed

Details : RTX (resiniferatoxin) is a small molecule which is act as TRPV1 agonist, which is investigated for the treatment of knee pain in moderate to severe osteoarthritis of the knee (OAK) patients.

Brand Name : RTX

Molecule Type : Small molecule

Upfront Cash : Not Applicable

September 07, 2023

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Details:

RTX is an intra-articular injection of resiniferatoxin developed for the treatment of pain in patients with moderate to severe pain associated with knee osteoarthritis.


Lead Product(s): Resiniferatoxin

Therapeutic Area: Rheumatology Brand Name: RTX

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable August 18, 2022

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02

Grunenthal

Germany
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Duphat
Not Confirmed

Grunenthal

Germany
arrow
Duphat
Not Confirmed

Details : RTX is an intra-articular injection of resiniferatoxin developed for the treatment of pain in patients with moderate to severe pain associated with knee osteoarthritis.

Brand Name : RTX

Molecule Type : Small molecule

Upfront Cash : Not Applicable

August 18, 2022

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Details:

The agreement includes competitive investment commitments for launch and commercialisation. Manufacturing and supply of RTX (resiniferatoxin) to Shionogi will be carried out exclusively by Grünenthal.


Lead Product(s): Resiniferatoxin

Therapeutic Area: Rheumatology Brand Name: RTX

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Shionogi

Deal Size: $670.0 million Upfront Cash: Undisclosed

Deal Type: Licensing Agreement August 04, 2022

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03

Grunenthal

Germany
arrow
Duphat
Not Confirmed

Grunenthal

Germany
arrow
Duphat
Not Confirmed

Details : The agreement includes competitive investment commitments for launch and commercialisation. Manufacturing and supply of RTX (resiniferatoxin) to Shionogi will be carried out exclusively by Grünenthal.

Brand Name : RTX

Molecule Type : Small molecule

Upfront Cash : Undisclosed

August 04, 2022

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Details:

Company begins enrollment in the phase 2 trial because data from the phase 1B of RTX (Resiniferatoxin) showed significant pain relief observed in patients with advanced OA disease and sustained pain relief last beyond 6 months.


Lead Product(s): Resiniferatoxin

Therapeutic Area: Musculoskeletal Brand Name: RTX

Study Phase: Phase IIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable December 07, 2021

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04

Duphat
Not Confirmed
Duphat
Not Confirmed

Details : Company begins enrollment in the phase 2 trial because data from the phase 1B of RTX (Resiniferatoxin) showed significant pain relief observed in patients with advanced OA disease and sustained pain relief last beyond 6 months.

Brand Name : RTX

Molecule Type : Small molecule

Upfront Cash : Not Applicable

December 07, 2021

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Details:

The Phase 1 was an ascending dose safety study in 17 patients to assess the safety and preliminary efficacy of epidural administration of resiniferatoxin for the treatment of intractable pain due to cancer.


Lead Product(s): Resiniferatoxin

Therapeutic Area: Neurology Brand Name: RTX

Study Phase: Phase IIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable October 13, 2021

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05

Duphat
Not Confirmed
Duphat
Not Confirmed

Details : The Phase 1 was an ascending dose safety study in 17 patients to assess the safety and preliminary efficacy of epidural administration of resiniferatoxin for the treatment of intractable pain due to cancer.

Brand Name : RTX

Molecule Type : Small molecule

Upfront Cash : Not Applicable

October 13, 2021

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Details:

The RTX clinical development program continues, with Phase 2 and 3 clinical trials planned in larger patient populations. The first Phase 2 trial will focus on identifying the recommended Phase 3 dose.


Lead Product(s): Resiniferatoxin

Therapeutic Area: Musculoskeletal Brand Name: MTX-071

Study Phase: Phase IIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable July 06, 2021

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06

Duphat
Not Confirmed
Duphat
Not Confirmed

Details : The RTX clinical development program continues, with Phase 2 and 3 clinical trials planned in larger patient populations. The first Phase 2 trial will focus on identifying the recommended Phase 3 dose.

Brand Name : MTX-071

Molecule Type : Small molecule

Upfront Cash : Not Applicable

July 06, 2021

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  • Deals

Details:

Mestex AG is a Swiss biotech company that has developed the innovative investigational medicine MTX-071 (resiniferatoxin) for the intra-articular treatment of pain associated with osteoarthritis of the knee.


Lead Product(s): Resiniferatoxin

Therapeutic Area: Neurology Brand Name: MTX-071

Study Phase: Phase IIProduct Type: Small molecule

Sponsor: Grunenthal

Deal Size: Undisclosed Upfront Cash: Undisclosed

Deal Type: Acquisition April 12, 2021

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07

Mestex AG

Country
arrow
Duphat
Not Confirmed

Mestex AG

Country
arrow
Duphat
Not Confirmed

Details : Mestex AG is a Swiss biotech company that has developed the innovative investigational medicine MTX-071 (resiniferatoxin) for the intra-articular treatment of pain associated with osteoarthritis of the knee.

Brand Name : MTX-071

Molecule Type : Small molecule

Upfront Cash : Undisclosed

April 12, 2021

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Details:

The Phase 1b trial was a placebo controlled ascending dose study with an open-label extension to assess the safety and preliminary efficacy of intra-articular administration of RTX or saline control for moderate to severe pain due to osteoarthritis of the knee.


Lead Product(s): Resiniferatoxin

Therapeutic Area: Neurology Brand Name: RTX

Study Phase: Phase IIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable September 28, 2020

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08

Duphat
Not Confirmed
Duphat
Not Confirmed

Details : The Phase 1b trial was a placebo controlled ascending dose study with an open-label extension to assess the safety and preliminary efficacy of intra-articular administration of RTX or saline control for moderate to severe pain due to osteoarthritis of th...

Brand Name : RTX

Molecule Type : Small molecule

Upfront Cash : Not Applicable

September 28, 2020

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Details:

This multicenter, open-label study enrolled 17 adults with intractable moderate to severe cancer pain. Subjects were treated with a one-time epidural administration of RTX at escalating dose level cohorts, ranging from 0.4 µg to 25 µg in 3 ml saline, in seven cohorts.


Lead Product(s): Resiniferatoxin

Therapeutic Area: Neurology Brand Name: RTX

Study Phase: Phase IProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable September 22, 2020

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09

Duphat
Not Confirmed
Duphat
Not Confirmed

Details : This multicenter, open-label study enrolled 17 adults with intractable moderate to severe cancer pain. Subjects were treated with a one-time epidural administration of RTX at escalating dose level cohorts, ranging from 0.4 µg to 25 µg in 3 ml saline, i...

Brand Name : RTX

Molecule Type : Small molecule

Upfront Cash : Not Applicable

September 22, 2020

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Details:

Safety in the higher dose cohort is expected to be supportive for testing RTX epidural administration in other advanced non-cancer disease related unmet clinical needs.


Lead Product(s): Resiniferatoxin

Therapeutic Area: Neurology Brand Name: Undisclosed

Study Phase: Phase IProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable February 27, 2020

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10

Duphat
Not Confirmed
Duphat
Not Confirmed

Details : Safety in the higher dose cohort is expected to be supportive for testing RTX epidural administration in other advanced non-cancer disease related unmet clinical needs.

Brand Name : Undisclosed

Molecule Type : Small molecule

Upfront Cash : Not Applicable

February 27, 2020

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ABOUT THIS PAGE

Resiniferatoxin Manufacturers

A Resiniferatoxin manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Resiniferatoxin, including repackagers and relabelers. The FDA regulates Resiniferatoxin manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Resiniferatoxin 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 Resiniferatoxin manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.

Resiniferatoxin Suppliers

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

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

Resiniferatoxin USDMF

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

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

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

Resiniferatoxin GMP

Resiniferatoxin 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 Resiniferatoxin 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 Resiniferatoxin GMP manufacturer or Resiniferatoxin GMP API supplier for your needs.

Resiniferatoxin CoA

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

Resiniferatoxin CoA mostly includes findings from lab analyses of a specific batch. For each Resiniferatoxin 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.

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