Frequently Asked Questions
What is ProThelial™ ?
ProThelial™ is polymerized cross-linked sucralfate malate paste. It forms a protective layer over the
oral mucosa by adhering to the mucosal surface which protect against
further irritation and relieves pain. The paste is used in the management of mouth lesions
of all types including stomatitis and mucositis caused by chemoradiation therapy.
ProThelial™ is indicated for the management (treatment and prevention) of oral mucositis
of any cause. Chemoradiation treatment for cancer is the most common cause of oral
mucositis, affecting approximately 400,000 individuals. ProThelial™ is the first
and only FDA-cleared polymerized sucralfate paste commercially available for oral mucositis.
What Is The Active Ingredient of ProThelial™ ?
The active ingredient of ProThelial™ is polymerized sucralfate cross-linked by calcium bound
malate. Malate can bind calcium at either end and the positively charged calcium cross-links
to several molecules of sucralfate. It is believed that this “cross-linking” action
polymerizes sucralfate into sheets of sucralfate that layer on the lining better than
non-polymerized sucralfate. These cross-linkages are not permanent but interchanging.
Is ProThelial™ A Medical Device Or A Drug?
Though ProThelial™ contains sucralfate, it is FDA cleared and marketed as a medical
device. Unlike a drug, a medical device has no chemical reaction to tissues of the body,
rather it treats or prevents disease by a mechanical mode of action. ProThelial™ uses a
mechanical mode of action to treat and prevent oral mucositis. As explained in ProThelial™MOA,
the cross-linked polymerization of sucralfate leads to improved adherence on the oral mucosa.
This improved adherence assists the body’s existing mechanisms for healing. These actions of
ProThelial™ are entirely mechanical or physical and not chemical as with a drug.
Does ProThelial™ Have Side Effects?
Sucralfate, the active ingredient of ProThelial™, does not cause serious side effects or adverse
reactions. Constipation has been traditionally reported by patients who take large oral doses of sucralfate.
Who Can Use ProThelial™?
Cancer treatment patients undergoing chemotherapy, radiation therapy, or both, who have a greater
than a 50% chance of developing mucositis should be prescribed ProThelial™.
How Do I Use ProThelial™?
Direction of use:
For Moderate Mucositis – 2.5 - 5 ml Dose
• For 1st day, administer dose every 8 hours.
• Then one dose every 12 hours.
For Severe Mucositis - 10 ml Dose
• Use 10 ml (2 teaspoons) of paste 3 times a day for the first 2 days.
• Then use 10 ml twice a day
Special Application Instructions
• Use tongue to apply paste throughout the mouth (as if using tongue to remove
peanut butter from teeth).
• ProThelial™ should be swished and gargled for 5 seconds, and then held in mouth
for 15 seconds.
• Then dose can be expectorated (or swallowed if so instructed by your physician).
• Alternatively, ProThelial™ may be applied with cotton-tipped swab to affected
areas of the oral mucosa.
How Long Should I Use ProThelial™ ?
ProThelial™ is to be used no longer than the time prescribed by the physician or licensed
practitioner, ideally no longer than the period of time wherein oral ulceration, irritation
or wound persists.
For patients receiving chemoradiation: ProThelial™ is to be used continuously during entire
course of treatment.
What Is The Maximal Daily Amount?
Maximal daily amount of ProThelial™ should not exceed 40 ml or 8 teaspoons.
How Can I Get It?
Federal law restricts ProThelial™ to sale by or on the order of a physician or properly
licensed practitioner.
What Is The Difference between ProThelial™ and Ordinary Sucralfate?
ProThelial™ (polymerized cross-linked sucralfate) is associated with 2-3 day reversal of
mucositis and regular sucralfate is not. Polymerized cross-linked sucralfate achieves and
maintains a surface concentration of sucralfate, three hours following administration, that
is 800% greater on normal mucosal lining and 2,400% greater on ulcerated mucosal lining
[ Kashimura K, Ozawa K (1999) Sucralfate Preparations. US Patent 5,968,906. Oct 19, 1999. ].
Chemically, standard potency sucralfate (such as Carafate, or generic sucralfate) is more
easily hydrated by water. Hydrated sucralfate remains in solution, making less of it
available for adherence to the lining. Polymerization with multi-dentate chelators convert
singular sucralfate into energetically stable sheets of sucralfate preferred over hydration
by water. Polymerized sheets of sucralfate are cross-linked by chelatable multivalent cations
which lead to energetically preferred pi-stacking (or pancaking) on to itself thereby
achieving and maintaining high surface concentrations of sucralfate. Pi-stacking is a
phenomenon common to electro-dense compounds [ McGaughey GB, Gagnes M, Rappe AK (1998)
Pi-stacking interactions. J Biol Chem 273(25): 15458-15463; Ma JC, Dougherty DA. The
Cation-Pi interaction (1997) Chem Rev 97:1303-1324. ], which sucralfate is, and which sucralfate
sheets exaggerate.
What If ProThelial™ Is Accidentally Swallowed?
ProThelial™ is not intended for ingestion but for the management of oral ulcerations, oral
irritations or oral mucosal wounds. However, ProThelial™ is safe if swallowed in doses up to 4
grams daily for 56 days.
Physician Swallow Evaluation: Any clinician prescribing ProThelial™ should evaluate the adequacy
of the patient’s ability to swallow to minimize any unintended incidental ingestion.
Are There Any Special Precautions?
Do not use any product jar that is not intact or is otherwise damaged in any way. Avoid eating
or drinking for at least 1 hour after use.
