Revertive
Revertive Uses, Dosage, Side Effects, Food Interaction and all others data.
Revertive is a glucagon-like peptide-2 (GLP-2) analogue. It is made up of 33 amino acids and is manufactured using a strain of Escherichia coli modified by recombinant DNA technology. Revertive differs from GLP-2 by one amino acid (alanine is substituted by glycine). The significance of this substitution is that teduglutide is longer acting than endogenous GLP-2 as it is more resistant to proteolysis from dipeptidyl peptidase-4. FDA approved on December 21, 2012.
An enhancement of gastrointestinal fluid absorption (750-1000 mL/day) was observed following daily administrations of teduglutide. An increase in villus height and crypt depth of the intestinal mucosa was also noted. A decrease in fecal weight has also been observed. Revertive does not prolong the QTc interval.
| Trade Name | Revertive |
| Availability | Prescription only |
| Generic | Teduglutide |
| Teduglutide Other Names | (Gly2)GLP-2, Glucagon-like peptide II (2-glycine) (human), Gly(2)-GLP-2, Teduglutida, Teduglutide, Teduglutide [rDNA origin], Teduglutide Recombinant |
| Related Drugs | somatropin, glutamine, Gattex |
| Type | |
| Formula | C164H252N44O55S |
| Weight | 3752.0 Da |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Spain |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Revertive is a glucagon-like peptide-2 (GLP-2) analog used to treat patients with Short Bowel Syndrome (SBS) who require parenteral nutritional support.
Treatment of short bowel syndrome (SBS), malabsorption associated with the removal of the intestine, in adults patients who are dependent on parenteral support.
Revertive is also used to associated treatment for these conditions: Short Bowel Syndrome (SBS)
How Revertive works
Revertive is an analog of naturally occurring human glucagon-like peptide-2 (GLP-2), a peptide secreted by L-cells of the distal intestine in response to meals. GLP-2 increases intestinal and portal blood flow and inhibit gastric acid secretion. Revertive binds to the glucagon-like peptide-2 receptors located in enteroendocrine cells, subepithelial myofibroblasts and enteric neurons of the submucosal and myenteric plexus. This causes the release of insulin-like growth factor (IGF)-1, nitric oxide and keratinocyte growth factor (KGF). These growth factors may contribute to the increase in crypt cell growth and surface area of the gastric mucosa. Ultimately, absorption through the intestine is enhanced.
Toxicity
The most common adverse reactions (≥ 10%) across all studies with GATTEX are abdominal pain, injection site reactions, nausea, headaches, abdominal distension, upper respiratory tract infection. In addition, vomiting and fluid overload were reported in the SBS studies (1 and 3) at rates ≥ 10%.
Food Interaction
No interactions found.[Moderate] MONITOR: Revertive has the potential to increase absorption of concomitantly administered oral medications.
Altered mental status in association with teduglutide treatment has been observed in patients on benzodiazepines in clinical trials.
In one case, a patient who received prazepam with teduglutide 0.05 mg She was admitted to the intensive care unit, where her benzodiazepine level was found to exceed 300 mcg Both medications were discontinued, and the coma resolved five days later.
MANAGEMENT: Careful monitoring and possible dosage adjustment of oral medications that require titration or have a narrow therapeutic index are recommended during coadministration with teduglutide.
Revertive Disease Interaction
Moderate: biliary and pancreatic disease, congestive heart failure, intestinal obstruction, liver impairment, neoplasias, renal impairment
Volume of Distribution
Vd, healthy subjects = 103 mL/kg
Elimination Route
The pharmacokinetic profile of teduglutide (when administered subcutaneously) is described by a one-compartment model with first order absorption in the abdomen, arm, and thigh. With escalating doses, teduglutide demonstrates linear pharmacokinetics.
Absolute bioavailability, SubQ = 88%;
Tmax, SubQ = 3-5 hours;
Cmax, 0.05 mg/kg SubQ, SBS patients = 36 ng/mL;
AUC, 0.05 mg/kg SubQ, SBS patients = 0.15 µg•hr/mL;
Revertive does not accumulate following multiple subcutaneous administrations.
Half Life
Terminal half-life, healthy subjects = 2 hours; Terminal half-life, SBS patients = 1.3 hours
Clearance
Plasma clearance, healthy subjects = 123 mL/hr/kg; This value indicates that teduglutide is primarily cleared by the kidney.
Elimination Route
Urine
Innovators Monograph
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