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Also known as: 879085-55-9, Gdc-0449, Erivedge, 2-chloro-n-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide, Vismodegib (gdc-0449), Hhantag691
Molecular Formula
C19H14Cl2N2O3S
Molecular Weight
421.3  g/mol
InChI Key
BPQMGSKTAYIVFO-UHFFFAOYSA-N
FDA UNII
25X868M3DS

Vismodegib
Vismodegib is an orally bioavailable, small molecule inhibitor of SMO and the Hedgehog (Hh) pathway, with potential antineoplastic activity. Upon oral administration, vismodegib targets, binds to and inhibits the cell membrane-spanning G-protein coupled receptor SMO, which may result in the suppression of Hh pathway signaling and a decrease in tumor cell proliferation and survival. SMO is activated upon binding of Hh ligand to the cell surface receptor Patched (PTCH); inappropriate activation of Hh signaling and uncontrolled cellular proliferation may be associated with SMO mutations.
Vismodegib is a Hedgehog Pathway Inhibitor. The mechanism of action of vismodegib is as a Smoothened Receptor Antagonist.
1 2D Structure

Vismodegib

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
2-chloro-N-(4-chloro-3-pyridin-2-ylphenyl)-4-methylsulfonylbenzamide
2.1.2 InChI
InChI=1S/C19H14Cl2N2O3S/c1-27(25,26)13-6-7-14(17(21)11-13)19(24)23-12-5-8-16(20)15(10-12)18-4-2-3-9-22-18/h2-11H,1H3,(H,23,24)
2.1.3 InChI Key
BPQMGSKTAYIVFO-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CS(=O)(=O)C1=CC(=C(C=C1)C(=O)NC2=CC(=C(C=C2)Cl)C3=CC=CC=N3)Cl
2.2 Other Identifiers
2.2.1 UNII
25X868M3DS
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Erivedge

2. Gdc 0449

3. Gdc-0449

4. Gdc0449

5. Hhantag691

6. Nsc 747691

7. Nsc-747691

8. Nsc747691

9. R 3616

10. R-3616

11. R3616 Cpd

12. Rg 3616

13. Rg-3616

14. Rg3616

2.3.2 Depositor-Supplied Synonyms

1. 879085-55-9

2. Gdc-0449

3. Erivedge

4. 2-chloro-n-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide

5. Vismodegib (gdc-0449)

6. Hhantag691

7. Gdc0449

8. Gdc 0449

9. Gdc-0449 (vismodegib)

10. Nsc-747691

11. Nsc-755986

12. 2-chloro-n-[4-chloro-3-(pyridin-2-yl)phenyl]-4-(methylsulfonyl)benzamide

13. Chembl473417

14. Chebi:66903

15. 2-chloro-n-(4-chloro-3-pyridin-2-ylphenyl)-4-methylsulfonylbenzamide

16. 25x868m3ds

17. Nsc755986

18. 2-chloro-n-[4-chloro-3-(2-pyridinyl)phenyl]-4-(methylsulfonyl)benzamide

19. 2-chloro-n-(4-chloro-3-(2-pyridinyl)phenyl)-4-(methylsulfonyl)benzamide

20. 2-chloro-n-(4-chloro-3-pyridin-2-yl-phenyl)-4-methanesulfonyl-benzamide

21. 2-chloro-n-[4-chloro-3-(pyridin-2-yl)phenyl]-4-methanesulfonylbenzamide

22. Benzamide, 2-chloro-n-(4-chloro-3-(2-pyridinyl)phenyl)-4-(methylsulfonyl)-

23. 2-chloranyl-~{n}-(4-chloranyl-3-pyridin-2-yl-phenyl)-4-methylsulfonyl-benzamide

24. Erivedge (tn)

25. Vismodegib [usan]

26. Vismodegib [usan:inn]

27. Nsc 747691

28. Vismodegibum

29. Unii-25x868m3ds

30. Hsdb 8130

31. R 3616

32. Nsc747691

33. Hh-antag691

34. Hhantag 691

35. Vismodegib, Free Base

36. Rg 3616

37. Rg-3616

38. Methanesulfonylbenzamide

39. Vismodegib [mi]

40. Vismodegib [inn]

41. Vismodegib (usan/inn)

42. Vismodegib [vandf]

43. Vismodegib; Gdc-0449

44. R-3616

45. Vismodegib [who-dd]

46. Gdc-0449 - Selumetinib

47. Mls006012035

48. Schembl302587

49. Gtpl6975

50. Vismodegib [orange Book]

51. Cur-691

52. Dtxsid40236689

53. Gdc-449

54. Bcpp000223

55. Hms3604k16

56. Hms3654e17

57. Bcp01715

58. Ex-a2178

59. Bdbm50249522

60. Mfcd12407408

61. Nsc755809

62. S1082

63. Zinc40899447

64. Gdc-0449,vismodegib, Hhantag691

65. 2-chloro-n-(4-chloro-3-(pyridin-2-yl)-phenyl)-4-(methylsulfonyl)benzamide

66. Akos015966534

67. Bcp9000713

68. Ccg-264811

69. Cs-0255

70. Db08828

71. Nsc-755809

72. Pb15086

73. Ncgc00242497-01

74. Ncgc00242497-02

75. Ncgc00242497-06

76. Ncgc00242497-12

77. Ac-26969

78. As-14066

79. Hy-10440

80. Smr004703564

81. Ft-0675833

82. Sw218087-2

83. Ec-000.2333

84. D09992

85. V-4050

86. Ab01565813_02

87. 085g559

88. Sr-01000941574

89. 2-chloro-n-[4-chloro-3-(pyridin-2-yl)phenyl]-4-

90. J-509076

91. Q2070286

92. Sr-01000941574-1

93. C538724000

94. 2-chloro-n-(4-chloro-3-(2-pyridl)phenyl)-4-(methylsulfonyl)benzamide

95. 2-chloro-n-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methyl Sulfonyl)benzamide

96. 2-chloro-n~1~-[4-chloro-3-(2-pyridyl)phenyl]-4-(methylsulfonyl)benzamide

97. 2-chloro-n-(4-chloro-3-pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide

98. 2-chloro-n-[4-chloro-3-(2-pyridinyl)phenyl]-4-(methylsulfonyl)-benzamide

99. Vis

2.4 Create Date
2008-05-12
3 Chemical and Physical Properties
Molecular Weight 421.3 g/mol
Molecular Formula C19H14Cl2N2O3S
XLogP33.8
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count4
Rotatable Bond Count4
Exact Mass420.0102189 g/mol
Monoisotopic Mass420.0102189 g/mol
Topological Polar Surface Area84.5 Ų
Heavy Atom Count27
Formal Charge0
Complexity625
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Information
1 of 2  
Drug NameErivedge
PubMed HealthVismodegib (By mouth)
Drug ClassesAntineoplastic Agent
Drug LabelVismodegib is an inhibitor of the hedgehog (Hh) signaling pathway, which is described chemically as 2-Chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide. The molecular formula is C19H14Cl2N2O3S. The molecular weight is 421.30 g/mo...
Active IngredientVismodegib
Dosage FormCapsule
RouteOral
Strength150mg
Market StatusPrescription
CompanyGenentech

2 of 2  
Drug NameErivedge
PubMed HealthVismodegib (By mouth)
Drug ClassesAntineoplastic Agent
Drug LabelVismodegib is an inhibitor of the hedgehog (Hh) signaling pathway, which is described chemically as 2-Chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide. The molecular formula is C19H14Cl2N2O3S. The molecular weight is 421.30 g/mo...
Active IngredientVismodegib
Dosage FormCapsule
RouteOral
Strength150mg
Market StatusPrescription
CompanyGenentech

4.2 Therapeutic Uses

Erivedge capsule is indicated for the treatment of adults with metastatic basal cell carcinoma, or with locally advanced basal cell carcinoma that has recurred following surgery or who are not candidates for surgery, and who are not candidates for radiation. /Included in US product label/

US Natl Inst Health; DailyMed. Current Medication Information for ERIVEDGE (vismodegib) capsule (January 2012). Available from, as of March 11, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=eb368bb6-80e3-4df9-8a85-91df0a2ada6a


4.3 Drug Warning

/BOXED WARNING/ WARNING: EMBRYO-FETAL DEATH AND SEVERE BIRTH DEFECTS ERIVEDGE (vismodegib) capsule can result in embryo-fetal death or severe birth defects. Erivedge is embryotoxic and teratogenic in animals. Teratogenic effects included severe midline defects, missing digits, and other irreversible malformations. Verify pregnancy status prior to the initiation of Erivedge. Advise male and female patients of these risks. Advise female patients of the need for contraception and advise male patients of the potential risk of Erivedge exposure through semen.

US Natl Inst Health; DailyMed. Current Medication Information for ERIVEDGE (vismodegib) capsule (January 2012). Available from, as of March 11, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=eb368bb6-80e3-4df9-8a85-91df0a2ada6a


Advise patients not to donate blood or blood products while receiving Erivedge and for at least 7 months after the last dose of Erivedge.

US Natl Inst Health; DailyMed. Current Medication Information for ERIVEDGE (vismodegib) capsule (January 2012). Available from, as of March 11, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=eb368bb6-80e3-4df9-8a85-91df0a2ada6a


Dysregulated hedgehog signaling is the pivotal molecular abnormality underlying basal-cell carcinomas. Vismodegib is a new orally administered hedgehog-pathway inhibitor that produces objective responses in locally advanced and metastatic basal-cell carcinomas. /The researchers/ tested the anti-basal-cell carcinoma efficacy of vismodegib in a randomized, double-blind, placebo-controlled trial in patients with the basal-cell nevus syndrome at three clinical centers from September 2009 through January 2011. The primary end point was reduction in the incidence of new basal-cell carcinomas that were eligible for surgical resection (surgically eligible) with vismodegib versus placebo after 3 months; secondary end points included reduction in the size of existing basal-cell carcinomas. In 41 patients followed for a mean of 8 months (range, 1 to 15) after enrollment, the per-patient rate of new surgically eligible basal-cell carcinomas was lower with vismodegib than with placebo (2 vs. 29 cases per group per year, P<0.001), as was the size (percent change from baseline in the sum of the longest diameter) of existing clinically significant basal-cell carcinomas (-65% vs. -11%, P=0.003). In some patients, all basal-cell carcinomas clinically regressed. No tumors progressed during treatment with vismodegib. Patients receiving vismodegib routinely had grade 1 or 2 adverse events of loss of taste, muscle cramps, hair loss, and weight loss. Overall, 54% of patients (14 of 26) receiving vismodegib discontinued drug treatment owing to adverse events. At 1 month, vismodegib use had reduced the hedgehog target-gene expression by basal-cell carcinoma by 90% (P<0.001) and diminished tumor-cell proliferation, but apoptosis was not affected. No residual basal-cell carcinoma was detectable in 83% of biopsy samples taken from sites of clinically regressed basal-cell carcinomas. Vismodegib reduces the basal-cell carcinoma tumor burden and blocks growth of new basal-cell carcinomas in patients with the basal-cell nevus syndrome. The adverse events associated with treatment led to discontinuation in over half of treated patients. Comment in The following popper user interface control may not be accessible. Tab to the next button to revert the control to an accessible version. Destroy user interface controlVismodegib in advanced basal-cell carcinoma.

PMID:22670904 Full text: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4362529 Tang JY et al; N Engl J Med 366 (23): 2180-8 (2012)


FDA Pregnancy Risk Category: D /POSITIVE EVIDENCE OF RISK. Studies in humans, or investigational or post-marketing data, have demonstrated fetal risk. Nevertheless, potential benefits from the use of the drug may outweigh the potential risk. For example, the drug may be acceptable if needed in a life-threatening situation or serious disease for which safer drugs cannot be used or are ineffective./

US Natl Inst Health; DailyMed. Current Medication Information for ERIVEDGE (vismodegib) capsule (January 2012). Available from, as of March 11, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=eb368bb6-80e3-4df9-8a85-91df0a2ada6a


For more Drug Warnings (Complete) data for Vismodegib (8 total), please visit the HSDB record page.


4.4 Drug Indication

Vismodegib is used for treating locally advanced or metastatic basal cell carcinoma in patients whose carcinoma has recurred after surgery, and in patients who are not candidates for surgery or radiation.


FDA Label


Erivedge is indicated for the treatment of adult patients with:

- symptomatic metastatic basal cell carcinoma

- locally advanced basal cell carcinoma inappropriate for surgery or radiotherapy


5 Pharmacology and Biochemistry
5.1 Pharmacology

Vismodegib selectively binds to and inhibits the transmembrane protein Smoothened homologue (SMO) to inhibit the Hedgehog signalling pathway.


5.2 FDA Pharmacological Classification
5.2.1 Active Moiety
VISMODEGIB
5.2.2 FDA UNII
25X868M3DS
5.2.3 Pharmacological Classes
Smoothened Receptor Antagonists [MoA]; Hedgehog Pathway Inhibitor [EPC]
5.3 ATC Code

L01XX43


L01XX43

S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355


L - Antineoplastic and immunomodulating agents

L01 - Antineoplastic agents

L01X - Other antineoplastic agents

L01XJ - Hedgehog pathway inhibitors

L01XJ01 - Vismodegib


5.4 Absorption, Distribution and Excretion

Absorption

The absolute bioavailability of a single dose is 31.8%. Absorption is saturable and is not affected by food.


Route of Elimination

Vismodegib is mostly excreted unchanged, and the main route of elimination is by the feces (82%) and the urine accounts for 4.4%.


Volume of Distribution

Vismodegib has a volume of distribution of 16.4 to 26.6 L.


The volume of distribution of vismodegib ranges from 16.4 to 26.6 L. Vismodegib plasma protein binding in patients is greater than 99%. Vismodegib binds to both human serum albumin and alpha-1-acid glycoprotein (AAG) and binding to AAG is saturable.

US Natl Inst Health; DailyMed. Current Medication Information for ERIVEDGE (vismodegib) capsule (January 2012). Available from, as of March 11, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=eb368bb6-80e3-4df9-8a85-91df0a2ada6a


The single dose absolute bioavailability of vismodegib is 31.8%. Absorption is saturable as evidenced by the lack of dose proportional increase in exposure after a single dose of 270 mg or 540 mg vismodegib. Erivedge capsule may be taken without regard to meals because the systemic exposure of vismodegib at steady state is not affected by food.

US Natl Inst Health; DailyMed. Current Medication Information for ERIVEDGE (vismodegib) capsule (January 2012). Available from, as of March 11, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=eb368bb6-80e3-4df9-8a85-91df0a2ada6a


Vismodegib and its metabolites are eliminated primarily by the hepatic route with 82% of the administered dose recovered in the feces and 4.4% recovered in urine.

US Natl Inst Health; DailyMed. Current Medication Information for ERIVEDGE (vismodegib) capsule (January 2012). Available from, as of March 11, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=eb368bb6-80e3-4df9-8a85-91df0a2ada6a


While recent publications have suggested the pharmacokinetics (PK) of vismodegib appear to be non-linear, there has not been a report describing the mechanisms of non-linearity. This study provides evidence that two separate processes, namely, solubility-limited absorption and concentration-dependent plasma protein binding, can explain the non-linear PK of vismodegib. This study provides quantitative results which can account for the lower than expected accumulation of vismodegib with continuous daily dosing. Vismodegib has demonstrated clinical activity in patients with advanced basal cell carcinoma. The pharmacokinetics (PK) of vismodegib are non-linear. The objective of this study was to determine whether vismodegib PK change following repeated dosing by administering a tracer intravenous (iv) dose of (14) C-vismodegib with single and multiple oral doses. Healthy post menopausal female subjects (n= 6/group) received either a single or daily 150 mg vismodegib oral dose with a (14) C-labelled 10 ug iv bolus dose administered 2 hr after the single or last oral dose (day 7). Plasma samples were assayed for vismodegib by LC-MS/MS and for (14) C-vismodegib by accelerator mass spectrometry. Following a single i.v. dose, mean clearance, volume of distribution and absolute bioavailability were 43.4 mL hr(-1) , 16.4 l and 31.8%, respectively. Parallel concentration-time profiles following single oral and i.v. administration of vismodegib indicated elimination rate limited PK. Following iv administration at steady-state, mean clearance and volume of distribution were 78.5 mL hr(-1) and 26.8 L, respectively. Comparison of iv PK parameters after single and multiple oral dosing showed similar half-life, increased clearance and volume of distribution (81% and 63% higher, respectively) and decreased bioavailability (77% lower) after repeated dosing. Relative to single dose, the unbound fraction of vismodegib increased 2.4-fold with continuous daily dosing. Vismodegib exhibited a long terminal half-life after oral and iv administration, moderate absolute bioavailability and non-linear PK after repeated dosing. Results from this study suggest that the non-linear PK of vismodegib result from two separate, non-linear processes, namely solubility limited absorption and high affinity, saturable plasma protein binding.

PMID:22458643 Full text: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3495143 Graham RA et al; Br J Clin Pharmacol 74 (5): 788-96 (2012)


For more Absorption, Distribution and Excretion (Complete) data for Vismodegib (7 total), please visit the HSDB record page.


5.5 Metabolism/Metabolites

The main metabolic enzymes are CYP2C9 and CYP3A4, however more than 98% of total systemic vismodegib is not metabolized. Metabolic pathways of vismodegib in humans include oxidation, glucuronidation, and pyridine ring cleavage. The two most abundant oxidative metabolites recovered in feces are produced in vitro by recombinant CYP2C9 and CYP3A4/5.


Greater than 98% of the total circulating drug-related components are the parent drug. Metabolic pathways of vismodegib in humans include oxidation, glucuronidation, and pyridine ring cleavage. The two most abundant oxidative metabolites recovered in feces are produced in vitro by recombinant CYP2C9 and CYP3A4/5.

US Natl Inst Health; DailyMed. Current Medication Information for ERIVEDGE (vismodegib) capsule (January 2012). Available from, as of March 11, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=eb368bb6-80e3-4df9-8a85-91df0a2ada6a


2-Chloro-N-(4-chloro-3-(pyridin-2-yl)-phenyl)-4-(methylsulfonyl)-benzamide (GDC-0449, vismodegib) is a potent and selective first-in-class small-molecule inhibitor of the Hedgehog signaling pathway and is currently in clinical development. In this study, we investigated the metabolic fate and disposition of GDC-0449 in rats and dogs after a single oral administration of (14)C-GDC-0449. ... GDC-0449 underwent extensive metabolism in rats and dogs with the major metabolic pathways being oxidation of the 4-chloro-3-(pyridin-2-yl)-phenyl moiety followed by phase II glucuronidation or sulfation. Three other metabolites resulting from an uncommon pyridine ring opening were found, mainly in feces, representing 1.7 to 17.7% of the dose in total in rats and dogs. ...

PMID:21363998 Yue Q et al; Drug Metab Dispos 39 (6): 952-65 (2011)


... Proposed metabolites from exploratory metabolite identification in vitro (rat, dog and human liver microsomes) and in vivo (dog and rat urine) include three primary oxidative metabolites (M1-M3) and three sequential glucuronides (M4-M6). Oxidative metabolites identified in microsomes M1 and M3 were formed primarily by P4503A4/5 (M1) and P4502C9 (M3). GDC-0449 was not a potent inhibitor of P4501A2, P4502B6, P4502D6, and P4503A4/5 with IC50 estimates greater than 20 uM. K(i)'s estimated for P4502C8, P4502C9 and P4502C19 and were 6.0, 5.4 and 24 uM, respectively. An evaluation with Simcyp suggests that GDC-0449 has a low potential of inhibiting P4502C8 and P4502C9. Furthermore, GDC-0449 (15 uM) was not a potent P-glycoprotein/ABCB1 inhibitor in MDR1-MDCK cells.

PMID:19845436 Wong H et al; Xenobiotica 39 (11): 850-61 (2009)


5.6 Biological Half-Life

The half-life after a single dose is 12 days, and after continuous daily dosing is 4 days.


The estimated elimination half-life of vismodegib is 4 days after continuous once-daily dosing and 12 days after a single dose.

US Natl Inst Health; DailyMed. Current Medication Information for ERIVEDGE (vismodegib) capsule (January 2012). Available from, as of March 11, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=eb368bb6-80e3-4df9-8a85-91df0a2ada6a


5.7 Mechanism of Action

Mutations of the Hedgehog pathway may results in uncontrolled proliferation of skin basal cells. Vismodegib binds to and inhibits the transmembrane protein Smoothened homologue (SMO) to inhibit the Hedgehog signalling pathway.


Vismodegib is an inhibitor of the Hedgehog pathway. Vismodegib binds to and inhibits Smoothened, a transmembrane protein involved in Hedgehog signal transduction.

US Natl Inst Health; DailyMed. Current Medication Information for ERIVEDGE (vismodegib) capsule (January 2012). Available from, as of March 11, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=eb368bb6-80e3-4df9-8a85-91df0a2ada6a


Recent evidence from in vitro and in vivo studies has demonstrated that aberrant reactivation of the Sonic Hedgehog (SHH) signaling pathway regulates genes that promote cellular proliferation in various human cancer stem cells (CSCs). Therefore, the chemotherapeutic agents that inhibit activation of Gli transcription factors have emerged as promising novel therapeutic drugs for pancreatic cancer. GDC-0449 (Vismodegib), orally administrable molecule belonging to the 2-arylpyridine class, inhibits SHH signaling pathway by blocking the activities of Smoothened. The objectives of this study were to examine the molecular mechanisms by which GDC-0449 regulates human pancreatic CSC characteristics in vitro. GDC-0499 inhibited cell viability and induced apoptosis in three pancreatic cancer cell lines and pancreatic CSCs. This inhibitor also suppressed cell viability, Gli-DNA binding and transcriptional activities, and induced apoptosis through caspase-3 activation and PARP cleavage in pancreatic CSCs. GDC-0449-induced apoptosis in CSCs showed increased Fas expression and decreased expression of PDGFRa. Furthermore, Bcl-2 was down-regulated whereas TRAIL-R1/DR4 and TRAIL-R2/DR5 expression was increased following the treatment of CSCs with GDC-0449. Suppression of both Gli1 plus Gli2 by shRNA mimicked the changes in cell viability, spheroid formation, apoptosis and gene expression observed in GDC-0449-treated pancreatic CSCs. Thus, activated Gli genes repress DRs and Fas expressions, up-regulate the expressions of Bcl-2 and PDGFRa and facilitate cell survival. These data suggest that GDC-0499 can be used for the management of pancreatic cancer by targeting pancreatic CSCs.

PMID:22087285 Full text: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3210776 Singh BN et al; PLoS One. 2011;6(11):e27306. doi: 10.1371/journal.pone.0027306. Epub 2011


Hedgehog (Hh) signaling is involved in the pathogenesis of liver fibrosis. It has been previously shown that Hh-inhibitor cyclopamine (CYA) can reduce liver fibrosis in rats. However, CYA is not stable in vivo, which limits its clinical application. This study compares the antifibrotic potential of two known Hh antagonists, vismodegib (GDC-0449, abbreviated to GDC) and CYA. GDC is a synthetic molecule presently in clinical cancer trials and has been reported to be safe and efficacious. These drugs attenuated early liver fibrosis in common bile duct ligated rats, improved liver function, and prevented hepatic stellate cell (HSC) activation, thereby suppressing epithelial to mesenchymal transition (EMT). While both CYA and GDC increased the number of proliferating cell nuclear antigen positive liver cells in vivo, only CYA increased Caspase-3 expression in HSCs in rat livers, suggesting that while GDC and CYA effectively attenuate early liver fibrosis, their hepatoprotective effects may be mediated through different modes of action. Thus, GDC has the potential to serve as a new therapeutic agent for treating early liver fibrosis.

PMID:22994359 Pratap A et al; J Drug Target 20 (9): 770-82 (2012)


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Omgene Life Sciences Pvt. Ltd

India

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

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Cosmoprof India
Not Confirmed
  • fda
  • EDQM
  • WHO-GMP

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USDMF CEP/COS JDMF EU-WC NDC KDMF VMF Others AUDIT
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04

Deva Holding AS

Turkey

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

Cosmoprof India
Not Confirmed
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05

Hetero Drugs

India

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

Cosmoprof India
Not Confirmed
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Hetero Drugs

India

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

arrow
Cosmoprof India
Not Confirmed
USDMF CEP/COS JDMF EU-WC NDC KDMF VMF Others AUDIT
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06

Hebei Huarong Pharmaceutical

China

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

Cosmoprof India
Not Confirmed
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Hebei Huarong Pharmaceutical

China

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

arrow
Cosmoprof India
Not Confirmed
USDMF CEP/COS JDMF EU-WC NDC KDMF VMF Others AUDIT
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07

DEAFARMA

Italy

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

Cosmoprof India
Not Confirmed
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DEAFARMA

Italy

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

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Cosmoprof India
Not Confirmed
USDMF CEP/COS JDMF EU-WC NDC KDMF VMF Others AUDIT
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08

Arevipharma

Germany

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

Cosmoprof India
Not Confirmed
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09

Alembic Pharmaceuticals Limited

India

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

Cosmoprof India
Not Confirmed
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API Reference Price

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[{"dataSource":"API Export","activeIngredients":"VISMODEGIB","year":"2021","qtr":"Q1","strtotime":1616005800,"product":"VISMODEGIB (GROUP:B) (TAX INVOICE NO:190 5205311 DATE:16.03.2021","address":"8-3-167\/D\/16, KALYAN NAGAR - I,VENGAL RAO NAGAR","city":"HYDERABAD, A.P.","supplier":"MSN LABORATORIES","supplierCountry":"INDIA","foreign_port":"DUBAI","customer":"GULF AGENCY COMPANY ","customerCountry":"UNITED ARAB EMIRATES","quantity":"1.00","actualQuantity":"1","unit":"KGS","unitRateFc":"39548.7","totalValueFC":"39140.5","currency":"USD","unitRateINR":2849480,"date":"18-Mar-2021","totalValueINR":"2849480","totalValueInUsd":"39140.5","indian_port":"HYDERABAD AIR","hs_no":"29339910","bill_no":"9459799","productDescription":"API","marketType":"LESS REGULATED MARKET","country":"UNITED ARAB EMIRATES","selfForZScoreResived":"Pharma Grade","supplierPort":"HYDERABAD AIR","supplierAddress":"8-3-167\/D\/16, KALYAN NAGAR - I,VENGAL RAO NAGAR, HYDERABAD, A.P.","customerAddress":""}]
18-Mar-2021
18-Mar-2021
KGS
overview
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Average Price (USD/KGS)

Number of Transactions

Total Quantity (KGS)

Total Value (USD)

Quantity (KGS) & Unit rate (USD/KGS) over time

API Imports and Exports

Importing Country Total Quantity
(KGS)
Average Price
(USD/KGS)
Number of Transactions

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FDF Dossiers

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01

F. Hoffmann-La Roche

Switzerland
AES 2024
Not Confirmed
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F. Hoffmann-La Roche

Switzerland
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AES 2024
Not Confirmed

vismodegib

Brand Name : Erivedge

Dosage Form : KAPSEL, HÅRD

Dosage Strength : 150 MG

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Sweden

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02

F. Hoffmann-La Roche

Switzerland
AES 2024
Not Confirmed
arrow

F. Hoffmann-La Roche

Switzerland
arrow
AES 2024
Not Confirmed

Hhantag691

Brand Name : Erivedge

Dosage Form : Vismodegib 150Mg 28 Combined Oral Use

Dosage Strength : 28 cps 150 mg bottle

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Italy

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03

F. Hoffmann-La Roche

Switzerland
AES 2024
Not Confirmed
arrow

F. Hoffmann-La Roche

Switzerland
arrow
AES 2024
Not Confirmed

Hhantag691

Brand Name : Erivedge

Dosage Form : Capsule, hard

Dosage Strength : 150 mg

Packaging : Bottle

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Norway

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04

F. Hoffmann-La Roche

Switzerland
AES 2024
Not Confirmed
arrow

F. Hoffmann-La Roche

Switzerland
arrow
AES 2024
Not Confirmed

Vismodegibum

Brand Name : Erivedge

Dosage Form : Caps

Dosage Strength : 150mg

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Switzerland

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05

F. Hoffmann-La Roche

Switzerland
AES 2024
Not Confirmed
arrow

F. Hoffmann-La Roche

Switzerland
arrow
AES 2024
Not Confirmed

VISMODEGIB

Brand Name : ERIVEDGE

Dosage Form : CAPSULE

Dosage Strength : 150MG

Packaging : 28

Approval Date :

Application Number : 2409267

Regulatory Info : Prescription

Registration Country : Canada

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06

F. Hoffmann-La Roche

Switzerland
AES 2024
Not Confirmed
arrow

F. Hoffmann-La Roche

Switzerland
arrow
AES 2024
Not Confirmed

VISMODEGIB

Brand Name : ERIVEDGE

Dosage Form : CAP

Dosage Strength : 150mg

Packaging : 28X1mg

Approval Date :

Application Number :

Regulatory Info : Originator

Registration Country : South Africa

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07

F. Hoffmann-La Roche

Switzerland
AES 2024
Not Confirmed
arrow

F. Hoffmann-La Roche

Switzerland
arrow
AES 2024
Not Confirmed

vismodegib

Brand Name : Erivedge

Dosage Form :

Dosage Strength :

Packaging : 28

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Australia

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08

Genentech

U.S.A
AES 2024
Not Confirmed
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Genentech

U.S.A
arrow
AES 2024
Not Confirmed

VISMODEGIB

Brand Name : ERIVEDGE

Dosage Form : CAPSULE;ORAL

Dosage Strength : 150MG

Packaging :

Approval Date : 2012-01-30

Application Number : 203388

Regulatory Info : RX

Registration Country : USA

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Europe

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01

AES 2024
Not Confirmed
arrow
arrow
AES 2024
Not Confirmed

vismodegib

Brand Name : Erivedge

Dosage Form : KAPSEL, HÅRD

Dosage Strength : 150 MG

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Sweden

blank

02

AES 2024
Not Confirmed
arrow
arrow
AES 2024
Not Confirmed

Hhantag691

Brand Name : Erivedge

Dosage Form : Vismodegib 150Mg 28 Combined Oral Use

Dosage Strength : 28 cps 150 mg bottle

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Italy

blank

03

AES 2024
Not Confirmed
arrow
arrow
AES 2024
Not Confirmed

Hhantag691

Brand Name : Erivedge

Dosage Form : Capsule, hard

Dosage Strength : 150 mg

Packaging : Bottle

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Norway

blank

04

AES 2024
Not Confirmed
arrow
arrow
AES 2024
Not Confirmed

Vismodegibum

Brand Name : Erivedge

Dosage Form : Caps

Dosage Strength : 150mg

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Switzerland

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