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Kybella

Generic Name: Deoxycholic Acid
Class: Other Miscellaneous Therapeutic Agents
VA Class: 92:92
Chemical Name: (3α,5β,12α)-3,12-Dihydroxy-cholan-24-oic acid
Molecular Formula: C24H40O4
CAS Number: 83-44-3

Introduction

Cytolytic agent; causes focal adipocytolysis when injected into fat tissue.1 2 3 4 5

Uses for Kybella

Submental Convexity/Fullness

Improvement in the appearance of moderate to severe convexity or fullness associated with submental fat (“double chin”) in adults.1 2 3 5 6 7 8

Manufacturer states that efficacy and safety of deoxycholic acid for the treatment of sub-Q fat outside the submental region not established and that the drug is not recommended for such use.1

Kybella Dosage and Administration

General

  • Should be administered by a healthcare professional.1

  • Clinicians administering deoxycholic acid must understand the relevant submental anatomy and associated neuromuscular structures in the area involved and any alterations to the anatomy due to prior surgical or esthetic procedures.1

  • Evaluate individuals for other potential causes of submental convexity/fullness (e.g., thyromegaly, cervical lymphadenopathy) prior to administration.1 Carefully consider use in individuals with excessive skin laxity, prominent platysmal bands, or other conditions for which reduction in submental fat may result in an esthetically undesirable outcome.1

  • Use caution in individuals who have had prior surgical or esthetic treatment of the submental area.1 Changes in anatomy or landmarks or the presence of scar tissue may affect the ability to safely administer deoxycholic acid or obtain the desired esthetic results.1

  • Premedication with topical and/or injectable local anesthesia (e.g., lidocaine) or the use of ice/cold packs may enhance comfort.1 4

  • Palpate the submental area prior to each treatment session to ensure sufficient submental fat and to identify sub-Q fat between the dermis and platysma (preplatysmal fat) within the target treatment area.1 Tailor the number of injections and treatments to the individual's submental fat distribution and treatment goals.1

Administration

Sub-Q Administration

Do not dilute or admix deoxycholic acid injection with other compounds.1

Vials are for single use only; discard any remaining drug in vial following administration of intended dose.1

Prior to drug administration, outline the planned treatment area with a surgical pen and apply a 1-cm injection grid to mark the injection sites.1

Inject deoxycholic acid only within the target submental fat treatment area.1 Do not inject drug above the inferior border of the mandible or within a region defined by a 1–1.5-cm line below the inferior border (from the angle of the mandible to the mentum).1 2 3 (See Marginal Mandibular Nerve Injury under Cautions.) Avoid injection into other tissues (e.g., muscle, salivary glands, lymph nodes).1

Withdraw 1 mL of deoxycholic acid into a sterile 1-mL syringe using a large-bore needle; expel any air bubbles in the syringe barrel.1 Instruct the individual receiving the drug to tense the platysma.1 Pinch the submental fat and use a 30-gauge or smaller 0.5-inch needle to inject 0.2 mL of deoxycholic acid into the preplatysmal fat next to each of the marked injection sites.1

Upon withdrawal of the needle, apply pressure to each injection site if needed to minimize bleeding; apply an adhesive dressing if needed.1

Do not inject the drug too superficially or withdraw the needle from the sub-Q fat during injection, as this may increase risk of intradermal exposure and potential skin ulceration.1

Avoid entry of deoxycholic acid into the postplatysmal fat by injecting the drug at a depth approximately mid-way into the sub-Q fat layer.1

If resistance is met during insertion of the needle indicating the possibility of contact with fascial or nonfat tissue, withdraw the needle to an appropriate depth before administering the drug.1

Dosage

Adults

Submental Convexity/Fullness
Sub-Q

2 mg/cm2.1

Prescribing Limits

Adults

Submental Convexity/Fullness
Sub-Q

May give up to 50 injections (0.2 mL each), or a total of 100 mg (10 mL), in a single treatment; may administer up to 6 single treatments at intervals of at least 1 month.1

Special Populations

Hepatic Impairment

Manufacturer currently makes no dosage recommendations for patients with hepatic impairment.1

Renal Impairment

Manufacturer currently makes no dosage recommendations for patients with renal impairment.1

Geriatric Patients

Use caution in dosage selection, starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.1

Cautions for Kybella

Contraindications

  • Presence of infection at injection sites.1

Warnings/Precautions

Marginal Mandibular Nerve Injury

Marginal mandibular nerve injury, manifested as an asymmetric smile or facial muscle weakness (paresis), reported in clinical trials; all such injuries in clinical trials resolved spontaneously.1 Do not inject deoxycholic acid into or in close proximity to the marginal mandibular branch of the facial nerve.1 (See Sub-Q Administration under Dosage and Administration.)

Dysphagia

Dysphagia reported in clinical trials in the setting of administration-site reactions (e.g., pain, swelling, induration of the submental area) and resolved spontaneously.1

Manufacturer states to avoid use of drug in individuals with current symptoms or history of dysphagia.1

Injection-Site Hematoma/Bruising

Use caution in individuals with bleeding abnormalities and in those currently being treated with antiplatelet or anticoagulant therapy as excessive bleeding or bruising in the treatment area may occur.1

Risk of Infection in Proximity to Vulnerable Anatomic Structures

To avoid potential tissue damage, do not inject into or near (within 1–1.5 cm) salivary glands, lymph nodes, or muscles.1

Specific Populations

Pregnancy

No adequate and well-controlled studies of deoxycholic acid in pregnant women.1

Lactation

Not known whether deoxycholic acid is distributed into milk.1

Pediatric Use

Safety and efficacy not established in individuals <18 years of age; manufacturer states that drug is not intended for use in children or adolescents.1

Geriatric Use

Insufficient experience in adults >65 years of age to determine whether geriatric individuals respond differently than younger adults.1 However, clinical experience generally has not revealed age-related differences.1

Hepatic Impairment

Data are lacking on the use of deoxycholic acid in patients with hepatic impairment.1

Common Adverse Effects

≥2% of deoxycholic acid recipients and more frequently than with placebo in 2 clinical trials: Injection-site reactions (edema/swelling,1 2 3 hematoma/bruising,1 2 3 pain,1 2 3 numbness,1 2 3 erythema,1 2 3 induration,1 2 3 paresthesia,1 2 3 nodule,1 2 3 pruritus,1 2 3 skin tightness,1 3 skin warmth,1 nerve injury),1 headache,1 2 3 oropharyngeal pain,1 hypertension,1 nausea,1 dysphagia.1

>20% of deoxycholic acid recipients: Injection-site edema/swelling,1 2 3 hematoma,1 2 3 pain,1 2 3 numbness,1 2 3 erythema,1 2 3 induration.1 2 3

Interactions for Kybella

Deoxycholic acid does not inhibit or induce CYP isoenzymes in vitro.1

Deoxycholic acid does not inhibit P-glycoprotein (P-gp); breast cancer resistance protein (BCRP); multidrug resistance-associated protein (MRP) 4 or MRP2; organic anion transport proteins (OATP) 1B1, 2B1, or 1B3; organic cation transporter (OCT) 1 or OCT2; organic anion transporter (OAT) 1 or OAT3; sodium taurocholate co-transporting polypeptide (NTCP); or apical sodium-dependent bile acid transporter (ASBT).1

Kybella Pharmacokinetics

Absorption

Bioavailability

Peak plasma deoxycholic acid concentrations achieved within a median of 18 minutes after single treatment dose of 100 mg.1

Duration

Deoxycholic acid plasma levels returned to the endogenous range within 24 hours after injection.1 4

Distribution

Plasma Protein Binding

Extensively (98%) bound to plasma proteins.1

Elimination

Metabolism

Under normal conditions, deoxycholic acid is not substantially metabolized.1

Elimination Route

Excreted intact in feces, along with endogenous deoxycholic acid.1

Stability

Storage

Parenteral

Solution for Injection

20–25°C ; excursions between 15–30°C permitted.1

Actions

  • Synthetic form of endogenous deoxycholic acid.1 2 4 7

  • Cytolytic drug; causes focal adipocytolysis when injected into sub-Q fat tissue.1 4 Resulting mild inflammatory response provokes macrophage infiltration into area, to remove cellular debris and released lipids.1 2 3 4 5 7

  • Albumin and tissue-associated protein attenuate the effects of deoxycholic acid, leaving skin and muscle largely unaffected.4 5 7

  • Endogenous deoxycholic acid is a component of bile; most of endogenous form is sequestered in enterohepatic circulation loop.1

Advice to Patients

  • Importance of advising individuals to read the manufacturer's patient information.1

  • Importance of individuals not receiving deoxycholic acid treatment if they have infection in the treatment area.1

  • Importance of individuals informing clinicians if they have had or plan to have surgery on the face, neck, or chin or have had cosmetic treatments in these areas; have had or have medical conditions in or near the neck area; have had or have trouble swallowing; or have bleeding problems.1

  • Importance of advising individuals about the possibility of serious adverse effects with deoxycholic acid treatment, including marginal mandibular nerve paresis (e.g., manifested as asymmetric smile, facial muscle weakness) or difficulty swallowing; importance of advising individuals to notify clinician if such manifestations develop or if any existing symptom worsens.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs or herbal supplements, especially anticoagulant or antiplatelet drugs.1

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of informing individuals receiving deoxycholic acid of other important precautionary information.1 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Deoxycholic acid

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

For sub-Q injection

10 mg/mL

Kybella (available in single-use vials)

Kythera Biopharmaceuticals

AHFS DI Essentials. © Copyright 2018, Selected Revisions February 5, 2018. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

1. Kythera Biopharmaceuticals. Kybella (deoxycholic acid) injection for subcutaneous use prescribing information. Westlake Village,CA; 2015 Apr. 

2. Jones H, Carruthers J, Joseph JH et al. REFINE-1, a multicenter, randomized, double/blind, placebo-controlled, phase 3 trial with ATX-101, an injectable drug for submental fat reduction. Dermatol Surg. 2016; 42:38-49. [PubMed 26673433]

3. Humphrey S, Sykes J, Kantor J. ATX-101 for reduction of submental fat: A phase III randomized controlled trial. J Am Acad Dermatol. 2016; 75(4):788-97. [PubMed 27430612]

4. Walker P, Fellmann J, Lizzul PF. A phase I safety and pharmacokinetic study of ATX-101: injectable, synthetic deoxycholic acid for submental contouring.. J Drugs Dermatol. 2015; 14(3):279-87. [PubMed 25738850]

5. McDiarmid J, Ruiz JB, Lee D. Results from a pooled analysis of two European, randomized, placebo-controlled, phase 3 studies of ATX-101 for the pharmacologic reduction of excess submental fat.. Aesthetic Plast Surg. 2014; 38(5):849-60. [PubMed 24984785]

6. Wollina U, Goldman A. ATX-101 for reduction of submental fat. Expert Opin Pharmacother. 2015; 16(5):755-62. [PubMed 25724831]

7. Rzany B, Griffiths T, Walker P. Reduction of unwanted submental fat with ATX-101 (deoxycholic acid), an adipocytolytic injectable treatment: results from a phase III, randomized, placebo-controlled study. Br J Dermatol. 2014; 170(2):445-53. [PubMed 24147933]

8. Ascher B, Hoffman K, Walker P. Efficacy, patient-reported outcomes and safety profile of ATX-101 (deoxycholic acid), an injectable drug for the reduction of unwanted submental fat: results from a phase III, randomized, placebo-controlled study.. J Eur Acad Dermatol Venereol. 2014; 28(12):1707-15. [PubMed 24605812]

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