griseofulvin

Trade name: grisactin

Small moleculeapproved

Approved

Aug 22, 1962

Griseofulvin is a mycotoxic metabolic product of Penicillium spp. It was the first available oral agent for the treatment of dermatophytoses and has now been used for more than forty years. Griseofulvin is fungistatic with in vitro activity against various species of Microsporum Epidermophyton, and Trichophyton. It has no effect on bacteria or on other genera of fungi. Following oral administration, griseofulvin is deposited in the keratin precursor cells and has a greater affinity for diseased tissue. The drug is tightly bound to the new keratin which becomes highly resistant to fungal invasions. Once the keratin-Griseofulvin complex reaches the skin site of action, it binds to fungal microtubules (tubulin) thus altering fungal mitosis. Griseofulvin is fungistatic, however the exact mechanism by which it inhibits the growth of dermatophytes is not clear. It is thought to inhibit fungal cell mitosis and nuclear acid synthesis. It also binds to and interferes with the function of spindle and cytoplasmic microtubules by binding to alpha and beta tubulin. It binds to keratin in human cells, then once it reaches the fungal site of action, it binds to fungal microtubes thus altering the fungal process of mitosis. — NCATS

Clinical trial activity

6 trials · 7 clinical orgs · 14 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Jun 1, 2004 (NCT00117767)

Timeline

1960s

Aug 22, 1962
Wyeth — Earliest FDA Approval
Aug 22, 1962
American Home Products — NDA Secondary Org
Aug 22, 1962
Wyeth — NDA Organization

1970s

Jul 14, 1971
Johnson and Johnson — Marketing Organization
Sep 9, 1971
Chartwell Pharmaceuticals — Marketing Organization
May 30, 1972
Johnson and Johnson — NDA Secondary Org
Jun 20, 1972
American Home Products — Marketing Organization
Apr 16, 1975
Bausch Health Companies — NDA Secondary Org

1980s

Jun 2, 1980
Bausch Health Companies — Marketing Organization

1990s

Jun 30, 1992
Pliva — Marketing Organization

2000s

Jan 1, 2004
Novartis — Earliest Phase 3 Sponsor(trial)
Jan 1, 2005
Actavis — Earliest Phase 1 Sponsor(trial)
Jul 6, 2007
Actavis — Marketing Organization
Sep 10, 2007
Cipla — Marketing Organization

2010s

Oct 8, 2010
Cosette — Marketing Organization
Oct 8, 2010
Vintage — Marketing Organization
Oct 22, 2012
Sigmapharm Laboratories — Marketing Organization
Aug 7, 2013
Sandoz — Marketing Organization
Aug 7, 2013
Novartis — Marketing Organization
Jan 9, 2014
Rocky Mountain Labs — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

TubulinINHIBITOR
Tubulin inhibitor
Binds to beta tubulin

Approval history

approvedAug 22, 1962

Chemistry & pharmacology

Loading structure…

SMILES

COC1=CC(OC)=C(Cl)C2=C1C(=O)[C@]3(O2)[C@H](C)CC(=O)C=C3OC

Mol. weight: 352.766 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Single Stereoisomer
Inorganic: No
Polymer: No
Delivery: Oral
Availability: Prescription Only

Oral

Yes

Parenteral

Topical

Sources

Also known as

amudane
amudane
curling factor
curling factor
fulcin
fulcin
fulcin
fulcin 125
fulcin 500
fulsovin
fulvicin
fulvicin
fulvicin
fulvicin p/g
fulvicin p/g
fulvicin-p/g
fulvicin-p/g
fulvicin p/g 165
fulvicin p/g 165
fulvicin p/g 330
fulvicin p/g 330
fulvicin-u/f
fulvicin-u/f
grifulvin
grifulvin
grifulvin
grifulvin v
grifulvin v
grisactin
grisactin
grisactin
grisactin ultra
grisactin ultra
grisefulin
griseofulvin
griseofulvin
griseofulvin
griseofulvin
griseofulvin
griseofulvin
griseofulvin
griseofulvin
griseofulvin
griseofulvin
(+)-griseofulvin
(+)-griseofulvin
(+)-griseofulvin
griseofulvina
griseofulvina
griseofulvine
griseofulvine
griseofulvin, microcrystalline
griseofulvin, microcrystalline
griseofulvin, microcrystalline
griseofulvin, microcrystalline
griseofulvin, microcrystalline
griseofulvin, microsize
griseofulvin, microsize
griseofulvin, microsize
griseofulvin, microsize
griseofulvin, ultramicrocrystalline
griseofulvin, ultramicrocrystalline
griseofulvin, ultramicrocrystalline
griseofulvin, ultramicrocrystalline
griseofulvin,ultramicrosize
griseofulvin,ultramicrosize
griseofulvin, ultramicrosize
griseofulvin, ultramicrosize
griseofulvin, ultramicrosize
griseofulvin, ultramicrosize
griseofulvin, ultramicrosize
griseofulvinum
griseofulvinum
grisol af
grisovin
grisovin
gris-peg
gris-peg
grivate
grysio
grysio
lamoryl
lamoryl
likuden
likuden
poncyl
poncyl
spirofulvin
spirofulvin
sporostatin
sporostatin
ultragris-165
ultragris-165
ultragris-330
ultragris-330

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT04318535	Phase 1	Jan 13, 2020	GlaxoSmithKline
NCT01518166	Phase 1	May 1, 2006	Novo Nordisk
NCT00863863	Phase 1	Jan 1, 2006	Actavis, Biovail
NCT00864071	Phase 1	Nov 1, 2005	Actavis, Biovail
NCT00127868	N/A	Mar 1, 2005	Chen, Catherine, M.D., Eastern Virginia Medical School
NCT00117767	Phase 3	Jun 1, 2004	Novartis

Showing 6 of 6 trials

Page 1 / 1

Organizations

Research & Development (7)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
Actavis	For profit	2	2	1	2005
Biovail	For profit	2	0	1	2005
Chen, Catherine, M.D.	Academic/Hospital	1	1	1	2005
Eastern Virginia Medical School	Academic/Hospital	1	0	1	2005
GlaxoSmithKline	For profit	1	1	1	2020
Novartis	For profit	1	1	1	2004
Novo Nordisk	For profit	1	1	1	2006

7 organizations

Page 1 / 1

Marketing (19)

Organization	Org type	Relationship	Date
Actavis	For profit	MKTG	Jul 6, 2007
American Home Products	For profit	NDA2	Aug 22, 1962
American Home Products	For profit	MKTG	Jun 20, 1972
Bausch Health Companies	For profit	NDA2	Apr 16, 1975
Bausch Health Companies	For profit	MKTG	Jun 2, 1980
Bausch Health Companies	For profit	SYN	Apr 16, 1975
Chartwell Pharmaceuticals	For profit	MKTG	Sep 9, 1971
Cipla	For profit	MKTG	Sep 10, 2007
Cosette	For profit	MKTG	Oct 8, 2010
Johnson and Johnson	For profit	NDA2	May 30, 1972
Johnson and Johnson	For profit	MKTG	Jul 14, 1971
Novartis	For profit	MKTG	Aug 7, 2013
Pliva	For profit	MKTG	Jun 30, 1992
Rocky Mountain Labs	Academic/Hospital	MKTG	Jan 9, 2014
Sandoz	For profit	MKTG	Aug 7, 2013
Sandoz	For profit	SYN	Aug 7, 2013
Sigmapharm Laboratories	For profit	MKTG	Oct 22, 2012
Vintage	For profit	MKTG	Oct 8, 2010
Wyeth	For profit	NDA	Aug 22, 1962